CS231212B1 - 2-R-3-R1 substituted benzothiazolium salt derivatives and processes for their preparation - Google Patents

2-R-3-R1 substituted benzothiazolium salt derivatives and processes for their preparation Download PDF

Info

Publication number
CS231212B1
CS231212B1 CS82688A CS68882A CS231212B1 CS 231212 B1 CS231212 B1 CS 231212B1 CS 82688 A CS82688 A CS 82688A CS 68882 A CS68882 A CS 68882A CS 231212 B1 CS231212 B1 CS 231212B1
Authority
CS
Czechoslovakia
Prior art keywords
methyl
preparation
salt derivatives
bromide
general formula
Prior art date
Application number
CS82688A
Other languages
Czech (cs)
Slovak (sk)
Other versions
CS68882A1 (en
Inventor
Viktor Sutoris
Vladimir Sekera
Jan Halgas
Original Assignee
Viktor Sutoris
Vladimir Sekera
Jan Halgas
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Viktor Sutoris, Vladimir Sekera, Jan Halgas filed Critical Viktor Sutoris
Priority to CS82688A priority Critical patent/CS231212B1/en
Publication of CS68882A1 publication Critical patent/CS68882A1/en
Publication of CS231212B1 publication Critical patent/CS231212B1/en

Links

Landscapes

  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Vynález sa týká nových látok 2^R-3-R substituovaných derivátov benzotiazóliových solí všeobecného vzorca I /■ (+) Podstata spdsobu přípravy látok podl’a vynálezu spočívá v tom, že derivát 2-R- -oenzotiazolu obecného vzorca II "2·θ—£ ” (ID reaguje so zlúčeninou obecného vzorca III r’x (III) Látky podl*e vynálezu mčžu nájsť uplatnenie ako agrochemikálie.The invention relates to new substances 2^R-3-R substituted derivatives of benzothiazolium salts of general formula I /■ (+) The essence of the method of preparing the substances according to the invention lies in the fact that the derivative of 2-R- -oensothiazole of general formula II "2·θ—£ ” (ID reacts with a compound of general formula III r’x (III) The substances according to the invention can find application as agrochemicals.

Description

231212 2

Vynález sa týká 2-R-3-R1 substituovaných derivátov benzotiazóliových solí obecnéhovzorce I

kde R znamená vodík, metyl; R1 znamená vodík, metyl, alyl, propargyl, butyl, etoxykarbonylmetyl, propoxykarbonylmetyl, alyloxykarbonylmetyl, benzyl, O / R znamená 4-metyl, 4-chlor, 6-metyl, 6-chlor a X znamená brómidovú, jódidovú, metylsulfátovú a hydrogensulfátovú skupinu a spSsobu leh přípravy. 2-R-3-R^-substituované benzotiazóliové soli a spčsob ich přípravy sú predmetomautorského osvedčenia č. 223 426. 2-R-3-R'-substituované deriváty benzotiazóliových solí podlá vynálezu nie sú v litera-tuře doteraz popísáné. Podobné žtúdiu biologickej účinnosti benzotiazóliových solí nebolado súčasnej doby věnovaná pozornost a len málo práč v tomto zmysle nachádzame u 2-substituo-vaných benzotiazóliových solí (Kendall J., Edwards H. D.: USA pat. 2 412 819; Chea. Abstr. 41. 5041 (1947); Garmalce D. L., Paris G. X., Komlossy J., Chambers C. H.,, Mc Grae R. C.: J. Med. Chem. 12.30 (1969)). Převážná část práč je věnovaná kondenzačným reakciám metylovej,resp. metylénovej skupině v polohe 2 s karbonylovými zlúčeninami a štúdiu priebehu reakclea reakčného prostredia (Deady 1. W.: Aust. J. Chem. 26. 1949 (1973); Deady L. W., Davis M.,Homfeld S., Aust. J. Chem. 27. 1917, 1221, (1974); Loches P., Meheux P., Neal J.: Bull.

Soc. Chim. Fr. 1968, 1093; Charbeurne D. J., Nunn A. J.: J. Chem. Soc. 1969, 4498).

Podstata spčsobu přípravy 2-R-3-R' substituovaných derivátov benzotiazóliových solipodl’a vynálezu spočívá v tom, že derivát 2-R-benzotiazólu obecného vzorca II, «ΜίθΰϊR (ID, o kde R a R majú význam uvedený hoře, reaguje so zlúčeninou obecného vzorca III, r’x (III), kde R1 a X majú význam uvedený hoře, v prostředí organických rozpúStadiel ako sú alifa-tické ketony s 1 až 4 atómami uhllka a dlmetylformamid, pri teplote 90 až 60 °C po dobu9 až 24 hodin.

Uvedená reakciu naznačuje nasledovná schéma:

kde R, r', R^ a x' je hoře uvedené 3 231212 Přikladl Všeobecný postup kvarternizácie benzotiazólu: 0,05 mol substituovaného benzotiazólua 0,06 mol halogénderivátu, resp. alkylsulfátu sa rozpustí v 12 ml bezvodej zmesi dimetyl-formamidu a acetonu (2:1). Reakčná zmes sa zahrieva na vodnom kúpeli s teplotou 50 až 60 °CAk po dvoch h nezačne krystalizovat kvartérna sol·, malé množstvo zmesi sa v skúmavke pre-myje petroléterom, potom acetónom a sklenou tyčinkou sa vyvolá kryštalizécia. Krystalickálátka sa vráti do reakčnej zmesi a pokračuje sa v zahrievaní óalšie 4 h. Po ochladeni sasol· odsaje, premyje bezvodým acetónom a krystalizuje z bezvodého tetrahydrofuránus 1 až 2 % metanolu. Výsledky elementérnej analýzy a fyzikálno-chemické konstanty syntetizovaných zlúčenínI - XVII sú uvedené v tabuTke 1. Látky podl’a vynálezu sú účinné ako inhibitory rastu.

Rastové testy boli realizované autormi modifikovanou metodou na modelovom objekteVika siata. Tento model bol vybraný pre vysokú homogenitu v klíčivosti semien a rastekllčencov. V sérii pokusov bola hl'adaná korelácia medzi štruktúrou, molaritou a biolo-gickou aktivitou. Příklad 2 bližšie osvetl’uje spfisob testovania zlúčenín I až XVII na inhibičnúúčinnost. Příklad 2 )

Semená Viky siatej sa nechajú klíčit v Petriho miskách v termostate v trne, pri 25 °C.

Klíčence po 48 h rastu boli exponované v molárnych roztokoch substituovaných benzetiazólío-i 2 vých solí, kde R, R , R a X podl’a všeobecného vzorce je uvedené v I až XVII tab. 1v koncentračnej škále 10”’^ až 10-’ M. Po 24 h inkubácii bol stanovený prírastok predTžo-vacieho rastu korenov. Pri každom stanovení bol uskutočnený aj rastový efekt v kontrolnejsérii. Šířka pokusného a kontrolného súboru, ako aj signifikantnosť medzi súbormi bolistanovené biometricky.

Ako Standard bol testovaný 2-chlóretyltrimetylamóniumchlorid (CGG). Výsledky inhi-bičného účinku zlúčenín I až XVII sú uvedené v tabuTke 2. 231212 4

3

N Φ 3 & t> Ό

O cx >9 tí

•H tí

JsQ 44

O *) co X» 5? tí

<D

P

P

M

XJ 0 Ř

CM

CA β •Μ r4 3

JO ¢0 >

O « ví

P ω ♦> « 0$

W Ví

»O

00 O IA IA Os Os CM IA H *« IA xř IA Os Os 44 CM 44 CM ·— *-» N M *4 O »64 O *4 >N *4 »4 *3 <0 k CO fc 0 Q> CO CO <0 IA CM Os lA rq cq CO OO r_ tA xT O xř IA M· IA OS Os CM CM CM os CM IA rq 00 IA kO t- t* 00 IA xr IA CM IA ť* xř t* CO IA — Xť m co 00 so CM OO 00 r- CO x* C— so e* 'M- M- rq O O — CO kO kO «- CM kO IA IA xt CO Os CO CO t* e* »- — rq cm T- CM CM *» O O «» T- CM CM CM CM CM CM o co — rq xř CM rq oo Os O0 rq CM cm rq co o co ř- o o CO os C* so ί— IA CM OS SO k£> kO rq ·- o vo SO xt Xf IA IA M· xt IA xř xfr xt 'M- IA IA IA IA CM O kO CO rq ia O Os O — cm rq 00 IA O os xf xt *- rq * OJ k0 xt xř rq rq rq IA rq cm rq rq xr xt rq rq CM CM rq rq rq rq Xt Xfr rq rq so ř- t* IA o CM CM IA os CM t- o r* O IA o — — CM CM OS IA Xf rq — IA xt SO IA Os so Os kO kO t* ř* xj- rq MJ \O kO SO CO so OS OS § $ sř s? rq rq rq rq xř rq rq rq rq rq rq rq rq kO SO \o kO t* M> ř- o o CM t*· IA t- v* CM CM M «1 M rq «» ** IA IA rq O O rq Ο» X* os kO OS o r~ c- CM CM CM CM CM CM rq CM CM CM CM CA CA xř CA Ώ £9 CM tA Q §? O ζΛ a CA rrt a 3 a s A h xfr gg h H Q Γ+ i-í n a O a O a O o CM CM a O o O O v* ·— nT . a~ OS £ W~ ’ Os c oo »£ Os a o a a o O o O o O o o o xfr O o ’φ CA CA o CA wP a aP íj &amp; W H a o a O H a a tP aP rí H H aP sf o o | V ? V O 1 v a M· xt xt Xfr a SO aP aP wf4 a O o tl lí H a a a o u O aP aP íP aP <*» a aP aP 3 a o o O o o O O o a a a a a a a a a H M H H w H > H H H H H H W H > > > H 5 231212

FokraSovanie tabulky

tA, OJ - to rn t—1 <7t ’Φ OJ OJ «a ,M Ol OJ 63 63 • >63 >63 • O >N O O *4 >64 P (0 (0 co CO <0 • 0 H O OJ σ\ σ» to O m c**· ·— OJ o co m to t- ’Φ O >N (0 OJ OJ Ol . 0 to to f* 0 0 Ot tO to to 10 lO to to f* S> XI)tí a oj ot C*~ Ol OJ O — f* OJ <- r*- «- 10 4) tO "Φ t- 10 10 t> 0 — OJ e* r- O <7\ 0 «- +>3£ a *« ·» Λ ~ u\ 0- to CO Ol OJ «— »— O\ « «. * 0 0 σ\ σ> O O\ 0 0 r— r~ σ\ Ot co w— «— e— «— N \ XD s pa Ή. — 0 Φ OJ to OJ "Φ ’Φ tO' 0 c- o- t* o\ t- 0 KJ# ia 10 «- 0 »- 0 01 «- μ· n Ol OJ co Ol m oj Ř s> Sot to ia 10 to *Φ ·φ ’Φ ’Φ ’Φ ’Φ ’Φ o r* Φ φ φ »- 00 t- Ol a to <J\ — co to to OJ — cq v- Ol 0 Ol OJ <x> a a a 1*1 v- Φ Φ φ m (0 5 m m 10 10 m m m m ’Φ Φ ’Φ φ φ co a 01 tO to m t- 10 m a c- ť- a f- co tO — 0 OJ 0 to cq OJ ΡΊ OJ r- a - to to to Ol ΓΊ Ol «“ r- ř- co od o> <A ř* t* t* t* <0 co to to M· *3· Μ- n m ’Φ ’Φ ’Φ ’Φ ’Φ IA 10 ΙΑ tO Λ tO ’ί· 10 ’Φ ia LA • Ol to OJ OJ 01 01 01 a ^J· Ol to 0 φ a 0 0 lO t* <n m J— Ol 01 Ol OJ Ol m m co m ΡΊ co co Ol 0 a co a a OJ OJ 0» >>o ω 0 0 0 co a fi Φ co a 0 a a a a * 0 a f-t a a &amp; á tS á á a m ca to OJ ’Φ φ 3 > 00 W5 a a a a a a a a 0 m OJ m to lA o 0 0 0 0 o 0 O 1 X b k h k &amp; © ta a a a a a a ro a o as a 1 OJ to co « H a O 1 OJ OJ 0 a a as 1 a » to aT o II o II to cn a a 10 8 0 0 a Ol OJ Ol 0 a a a 0 g 0 Ol 8 IA a IA a «a II 0 a 0 tO to Pí 0 σ» 0 0 O 0 0 0 Ol a Ol Ol OJ OJ Ol OJ a ’Φ a a a a a a « o o 0 0 o 0 0 /*> a 0 0 M a a a a a a H M * w H > H H n H H W H ► > > M H X X X X X X X »O 6 231212 Názov zlúčeniny: I Benzotiazóliumhydrogensulfát II 3-Metyl-4-metylbenzotiazóliumjodid III 3-Metyl-4-metylbenzotiazóliumbromid IV 3-Metyl-4-chlórbenzotiazóliummetosulfát V 3-Metyl-4-chlórbenzotiazóliumbromid VI 3-Metyl-6-chlórbenzotiazóliummetosulfát VII 3-Alylbenzotiazóliumjodid VIII 3-Alyl-4-metylbenzotiazóliumbromid IX 3-Alyl-6-metylbenzotiazóliumbromid X 3-Propargyl-6-nietylbenzotiazóliumbromld XI 3-Butylbenzotiazóliumbromid XII 3-Etoxykarbonylmetyl-6-chlórbenzotiazóliumbromid XIII 3-Propoxykarbonylmetyl-6-chlórbenzotiazóliumbromid XIV 3_Alyloxykarbonylmetylbenzotiazóliumbromid XV 3-Alyloxykarbonylmetyl-6-metylbenzotiazóliumbromid XVI 2-Metyl-3-benzylbenzotiazóliumbromid XVII 3-Benzyl-6-metylbenzotiazóliumbromid

Tabulka 2

Inhibičný účinok syntetizovaných zlúčenín podl’a vynálezu Číslo R R1 R2 X- Inhibicia (mm) M I II H H H CH3 H 4-CH3 HSO4 I 22,35 14,55 10'3 10‘3 III IV H H gh3 CH3 4-CH3 4-C1 Br ch3so4 14,60 19,20 10-3 10-3 10"3 v H CH, 4-C1 Br 19,15 VI VII VIII H H H CH3 CH2CH=CH2 ch2ch=ch2 6-C1 H 4-CHj ch3so4 I Br 5,65 20,00 7,40 10“3 10-3 10-3 IX H GH2CH=CH2 6-CH3 Br „ 10,00 ,0"3 10“’ 10“3 X XI H H ch2c=ch C4H9 H H Br Br 30,20 16,70 XII XIII H H CH2COOC2H5 C^C^COOCjfty 6-C1 H Br Br 9,80 2,00 10-3 10-13 XIV H ch?cooch;)ch=ch2 H Br 12,35 10-3 XV H gh?cooch?ch»gh2 6-CH3 Br 8,60 10-3 XVI gh3 ch2c6h5 H Br 3,00 10-5 XVII H ch2c6h5 6-CH3 Br 10,30 10“3

Standard: 2-ehlóretyltrimetylamóniumchlorid (CCG) 3,85 10-3 Látky podl’a vynálezu m6žu nájsť Široké uplatnenie v laboratórnej chemickej analýzea chemickom priemyšle, ale aj ako agrochemikálie.

231212 2

The invention relates to 2-R-3-R1 substituted benzothiazolium salt derivatives of general formula I

wherein R is hydrogen, methyl; R 1 is hydrogen, methyl, allyl, propargyl, butyl, ethoxycarbonylmethyl, propoxycarbonylmethyl, allyloxycarbonylmethyl, benzyl, O / R is 4-methyl, 4-chloro, 6-methyl, 6-chloro and X is bromide, iodide, methylsulfate and hydrogen sulfate groups and the preparation process. The 2-R-3-R 6 -substituted benzothiazolium salts and the method for their preparation are the subject of Certificate No. 223 426. The 2-R-3-R'-substituted benzothiazolium salt derivatives of the present invention are not yet described in the literature. A similar study of the biological efficacy of the benzothiazolium salts or of the present day attention and little in this regard is found in the 2-substituted benzothiazole salts (Kendall J., Edwards HD: U.S. Pat. No. 2,412,819; Chea. Abstr. 41, 5041 ( Garmalce DL, Paris GX, Komlossy J, Chambers CH, Mc Grae RC, J. Med Chem, 12.30 (1969). The major part of the washing machine is devoted to the condensation reactions of methyl, respectively. methylene group at position 2 with carbonyl compounds and study of reaction medium reaction (Deady 1st W. Aust. J. Chem. 26, 1949 (1973); Deady LW, Davis M., Homfeld S., Aust. J. Chem 27, 1917, 1221, (1974), Loches P., Meheux P., Neal J .: Bull.

Soc. Chim. Fr. 1968, 1093; Charbeurne DJ, Nunn AJ: J. Chem. Soc. 1969, 4498).

The process for preparing 2-R-3-R 'substituted benzothiazolium salt derivatives according to the invention is characterized in that the 2-R-benzothiazole derivative of the general formula II, «ΜίθΰϊR (ID, o where R and R are as defined above, reacts with a compound of formula III, r'x (III), wherein R 1 and X are as defined above, in an organic solvent environment such as aliphatic ketones of 1 to 4 carbon atoms and dlmethylformamide, at 90 to 60 ° C for 9 to 24 hours.

The following scheme suggests the following response:

wherein R 1, R 2, R 4 and R 3 'are as defined in 231212 Example 1 General procedure for the benzothiazole quaternization: 0.05 mol of substituted benzothiazole and 0.06 mol halogeno derivative, respectively. The alkyl sulfate was dissolved in 12 mL of an anhydrous mixture of dimethylformamide and acetone (2: 1). The reaction mixture is heated in a 50-60 ° C water bath, and after two hours the quaternary salt does not crystallize, a small amount of the mixture is washed with petroleum ether, then with acetone and a glass rod to crystallize. The crystalline product is returned to the reaction mixture and heating is continued for a further 4 h. After cooling, the sassol is suctioned off, washed with anhydrous acetone and crystallized from anhydrous tetrahydrofuran to 1-2% methanol. The results of the elemental analysis and the physico-chemical constants of the synthesized compounds I-XVII are shown in Table 1. The compounds of the invention are effective as growth inhibitors.

Growth tests were carried out by the authors by a modified method on the model object Vika siata. This model was chosen for high homogeneity in seed germination and seedlings. In a series of experiments, a correlation was found between structure, molarity and biological activity. Example 2 further illustrates the method of testing compounds I to XVII for potency inhibition. Example 2)

Seeds of Sika seed are germinated in Petri dishes in a thermostate in a thorn, at 25 ° C.

Germs after 48 h growth were exposed in molar solutions of substituted benzethiazolium salts, where R, R, R and X according to the general formula are given in I to XVII tab. 1 in a concentration range of 10 µM to 10 µM. After 24 h incubation, the increase in preload growth of the roots was determined. A growth effect in the control series was also performed for each assay. The width of the test and control sets as well as the significance between the sets was biometrically determined.

2-Chloroethyltrimethylammonium chloride (CGG) was tested as a standard. The results of the inhibitory effect of compounds I to XVII are shown in Table 2. 231212 4

3

N Φ 3 &amp;t> Ό

O cx> 9 th

• H thi

JsQ 44

O *) What X »5? tí

<D

P

P

M

XJ 0 Ø

CM

CA β • 4 r4 3

JO ¢ 0>

O «knows

P ω ♦> $ 0 $

W Ví

"O

O IA Os IA IA IA IA IA IA IA IA IA IA IA IA IA IA IA IA O O O O * * * * * * * * * * O O O O CO CO <0 IA CM IA rq cq COOO r_A xT O xI IA ·A OS OS CM CM CM os CM IA rq 00 IA kO - t * 00 IA xr IA CM IA ť * x t t * CO IA - X m co so so so r CO O O O O O O O O k - - - - - - - - - - k q q q q q q q q q q q q CM-CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM Q SO CM OS SO k £ k O · q x x x f f f f f f f f f f f---O O O O O O O r r r r r r r xt rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rt rfr rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq - IA xt SO IA Os os O k k t * xj-rq Q o SO CO with OS OS $ $ s? rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq rq X »Ο k Ο Ο Ο CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM Ώ Ώ Ώ Ώ Ώ Ώ O ζΛ and CA rrt a 3 as A h xfr gg h HQ Γ + i-í to O and O and O o CM CM and O o OO in * · - nT. ~ Os ~ Os Os Os CA CA CA CA CA CA CA CA CA CA CA CA CA CA CA w a a w a CA CA CA a CA wP and aP j &amp; WH α and OH and α and β and β HH aP sf ω V? VO 1 a M x x x x X a a p a p a p a p a p a p a p a p 3 a o 0 o o oaaaaaaaa h h h w h HHHHHHWH>> H 5 231212

Table Filling

,, - to to to 1 1 1 1 1 OJ OJ OJ OJ OJ 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 63 to »O mccccc OJccc · · · · · · · · · · · · · · · · · · · · · · · · í j j C * * OJ OJ O O O O O O O O O O O O O O O O - - - - "" 10 10 10 10 10 10 10 10 10 10 10 10 OJ A CO Ol Ol Ol Ol Ol Ol Ol Ol Ol----------co co co co co co co co co co co co co co «- N XD s pa - - 0 Φ to to""" Φ '''''0 0 0 0 0 0 0 J J J J J J J J J Co co 10 10 * 00 00 00 00 00 00 00 00 00 00 00 00 00 00 00 00 00 00 00 00 00 t- t- t- q q q q q q -Ol Ol Ol x ((((tO tO tO tO tO tO tO tO tO tO tO tO tO tO tO tO tO what - 0 OJ OJ OJ 0 «« «r co r r r--------· · · · · · · · 10- nm 'Φ' Φ 'Φ' Φ 'Φ IA 10 LA Ι' 10 '' • • • • • • • • • • • LA Ol to 01 01 01 01 01 J · to φ 01 0 0 0 — mm mm mm mm mm mm mm mm mm mm mm mm mm 01 01 01 01 01 ω ω 0 aaaa * 0 and ft aa &amp; tS á φ>>3> 00 W5 aaaaaaaa 0 m OJ m to lA o 0 0 0 0 o 0 O 1 X bkhk &amp; Aaaaaa ro aa a 1 o a o o o o o o o o o 0 aa a 1 o o aT o o o o o 0 o 0 a o 10 o 0 0 a o o o 0 aaa 0 g 0 o 8 aa a 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0/0> 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 H> HH n HHWH ►>> MHXXXXXXX »O 6 231212 Compound Name: I Benzothiazolium Hydrogen Sulfate II 3-Methyl-4-methylbenzothiazolium iodide III 3-Methyl-4-methylbenzothiazolium bromide IV 3-Methyl-4-chlorobenzothiazolium methoxide S 3-Methyl-4-chlorobenzothiazolium bromide VI 3-Methyl-6-chlorobenzothiazolium methosulfate VII 3-Allylbenzothiazolium iodide VIII 3-Allyl-4-methylbenzothiazolium bromide IX 3-Allyl-6-methylbenzothiazolium bromide X 3-Butylbenzothiazolium bromide XII 3-Ethoxycarbonylmethyl-6-chlorobenzothiazolium bromide XIII 3 -Propoxycarbonylmethyl-6-chlorobenzothiazolium bromide XIV 3-Allyloxycarbonylmethylbenzothiazolium bromide XV 3-Allyloxycarbonylmethyl-6-methylbenzothiazolium bromide XVI 2-Methyl-3-benzylbenzothium zolium bromide XVII 3-Benzyl-6-methylbenzothiazolium bromide

Table 2

Inhibitory effect of the synthesized compounds of the invention R 1 R 2 R 2 X- Inhibition (mm) MI II HHH CH 3 H 4-CH 3 HSO 4 I 22.35 14.55 10'3 10'3 III IV HH gh3 CH3 4-CH3 4- C1 Br ch3so4 14.60 19.20 10-3 10-3 10 "3 in H CH, 4-Cl Br 19.15 VI VII VIII HHH CH3 CH2CH = CH2 ch2ch = ch2 6-C1 H4-CH3 ch3so4 I Br 5,65 20,00 7,40 10 “3 10-3 10-3 IX H GH2CH = CH2 6-CH3 Br“ 10,00, 0 ”3 10“ 10 ”3 X XI HH ch2c = ch C4H9 HH Br Br 30.20 16.70 XII XIII HH CH2COOC2H5 C ^ C ^ COOCjfty 6-Cl H Br Br 9.80 2.00 10-3 10-13 XIV H chochoch;) ch = ch2 H Br 12.35 10 -3 XV H gh? Cooch? Ch »gh2 6-CH3 Br 8.60 10-3 XVI gh3 ch2c6h5 H Br 3.00 10-5 XVII H ch2c6h5 6-CH3 Br 10.30 10 '3

Standard: 2-chloroethyltrimethylammonium chloride (CCG) 3.85 10-3 The compounds of the invention may find wide application in the laboratory chemical analysis and chemical industry, but also as agrochemicals.

Claims (2)

7 231212 PREDMET VYNÁLEZU 1. 2-R-3-R1-substituované deriváty benzotiazóliových solí obecného vzorca I R7 231212 SUBJECT OF THE INVENTION 1. 2-R-3-R1-substituted benzothiazolium salt derivatives of Formula I R X ÍI), kde R znamená H a metyl, R1 znamená H, metyl, alyl, propargyl, butyl, etoxykarbonylmetyl, propoxykarbonylmetyl,. alyloxykarbonylmetyl, benzyl, 2 * * R znamená 4-metyl, 4-chlor, 6-metyl, 6-chlor, X znamená bromidovú, jodidovú, metylsulfátovd a hydrogénsulfátovú skupinu.X 1), wherein R is H and methyl, R 1 is H, methyl, allyl, propargyl, butyl, ethoxycarbonylmethyl, propoxycarbonylmethyl, and R 1 is hydrogen. allyloxycarbonylmethyl, benzyl, 2 * R is 4-methyl, 4-chloro, 6-methyl, 6-chloro, X is bromide, iodide, methylsulfate and hydrogen sulfate. 2. Spfisob přípravy látok podl’a bodu 1 vyznaíujúci sa tým, že derivát 2-R-benzotiazóluobecného vzorca II R2. Preparation of the substances according to item 1, characterized in that the 2-R-benzothiazole-general formula II R derivative -R (II), 2 kde R a R májá význam uvedený v bode 1reaguje so zlúčeninou obecného vzorca III r'x (III), kde R1 a X majú význam uvedený v bode 1, v prostředí organických rozpúšťadiel ako sú alifatické ketony s 1 až 4 atornami uhlíkaa dimetylformamid, pri teplote 50 až 60 °C po dobu 5 až 24 hodin. 4 1-R (II), wherein R and R are as defined in 1 above, with a compound of formula (III) wherein R 1 and X are as defined in 1, in an organic solvent such as aliphatic ketones of 1 up to 4 hours of carbon and dimethylformamide, at 50 to 60 ° C for 5 to 24 hours. 4 1
CS82688A 1982-02-02 1982-02-02 2-R-3-R1 substituted benzothiazolium salt derivatives and processes for their preparation CS231212B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CS82688A CS231212B1 (en) 1982-02-02 1982-02-02 2-R-3-R1 substituted benzothiazolium salt derivatives and processes for their preparation

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CS82688A CS231212B1 (en) 1982-02-02 1982-02-02 2-R-3-R1 substituted benzothiazolium salt derivatives and processes for their preparation

Publications (2)

Publication Number Publication Date
CS68882A1 CS68882A1 (en) 1984-03-20
CS231212B1 true CS231212B1 (en) 1984-10-15

Family

ID=5339464

Family Applications (1)

Application Number Title Priority Date Filing Date
CS82688A CS231212B1 (en) 1982-02-02 1982-02-02 2-R-3-R1 substituted benzothiazolium salt derivatives and processes for their preparation

Country Status (1)

Country Link
CS (1) CS231212B1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105461654A (en) * 2015-12-01 2016-04-06 南京林业大学 Benzothiazole ionic liquid and preparation method as well as application thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105461654A (en) * 2015-12-01 2016-04-06 南京林业大学 Benzothiazole ionic liquid and preparation method as well as application thereof

Also Published As

Publication number Publication date
CS68882A1 (en) 1984-03-20

Similar Documents

Publication Publication Date Title
FI81096B (en) FOERFARANDE FOER FRAMSTAELLNING AV TERAPEUTISKT ANVAENDBARA 2- (N-SUBSTITUERAD GUANIDINO) -4-HETEROARYLTIAZOLFOERENINGAR.
CA1172636A (en) Thiazolidinylalkylene piperazine derivatives
TW201938558A (en) Crystal form, salt type of pyridoimidazole compound and preparation method thereof
CS231212B1 (en) 2-R-3-R1 substituted benzothiazolium salt derivatives and processes for their preparation
SU1356962A3 (en) Method of producing derivatives of carbostyrene
NO136360B (en)
FI78074B (en) PROCEDURE FOR THE PREPARATION OF PHARMACOLOGICAL PROPERTIES OF SUBSTITUTES 2-PHENYL-2-PYRIDYLOXI-OCH-THIO-ETHYLAMINER.
PL126169B1 (en) Process for preparing novel derivatives of pyrimid-4-one
Sanfilippo et al. Synthesis of (aryloxy) alkylamines. I. Novel antisecretory agents with H+ K+-ATPase inhibitory activity
Marcincal-Lefebvre et al. (Phenylthio) phenylamine derivatives as potential antiinflammatory compounds
FI64800B (en) FOERFARANDE FOER FRAMSTAELLNING AV ISOTIOURINAEMNEDERIVAT ANVAENDBARA SOM HISTAMIN H2-ANTAGONISTER
US4777256A (en) 5-halopyridine-3-carboxamide compounds
PL95852B1 (en) METHOD OF MAKING NEW ACYLATED DERIVATIVES OF 2-AMINOTHIAZOLES
US2676968A (en) Aralkylphenoxyacetamidine and derivatives thereof
Lampe et al. Cardiotonic agents. 6. Histamine analogs as potential cardiovascular selective H2 agonists
Swensen et al. Organic Fungicides. III. The Preparation of Some α, α-Dichloroacetamides
PL126790B1 (en) Method of obtaining new derivatives of guanidine
SE464302B (en) ETHANIIMIDAMIDES AS INTERMEDIATES FOR THE PREPARATION OF HISTAMIN -H2 RECEPTOR ANTAGONISTS AND PROCEDURES FOR THE PRODUCTION OF THEREOF
US3074954A (en) Heterocyclic compounds
CH647518A5 (en) METHOD FOR PRODUCING BUSPIRON.
Allam et al. Activated nitriles in heterocyclic synthesis: Facile synthesis of heteroarylthymine analogs and their nucleosides
FI58125C (en) PROCEDURE FOR FRAMSTATING AV 6,7-DIMETOXY-4-AMINO-2- (4- (2-FUROYL) -1-PIPERAZINYL) QUINAZOLINE WITH BLODTRYCKSSAENKANDE VEKAN
Zuliani et al. The role of HB-donor groups in the heterocyclic polar fragment of H3-antagonists.: I. Synthesis and biological assays
Richter Development of the Solution-Spray Flash-Vacuum-Pyrolysis Technique in the Synthesis of Allenyl Isothiocyanates and Synthesis of Complex 2-Amino-1, 3-thiazole Derivatives
Gueremy et al. 4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for. alpha. 2-adrenoceptors