CH357722A - Process for the preparation of a new hydrazine derivative - Google Patents

Process for the preparation of a new hydrazine derivative

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Publication number
CH357722A
CH357722A CH357722DA CH357722A CH 357722 A CH357722 A CH 357722A CH 357722D A CH357722D A CH 357722DA CH 357722 A CH357722 A CH 357722A
Authority
CH
Switzerland
Prior art keywords
hydrazine
methyl
piperidyl
isopropylidene
solution
Prior art date
Application number
Other languages
German (de)
Inventor
Ernst Dr Jucker
Erwin Dr Rissi
Rudolf Dr Sueess
Arnold Dr Vogel
Eberhard Dr Wolff
Original Assignee
Sandoz Ag
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 Sandoz Ag filed Critical Sandoz Ag
Publication of CH357722A publication Critical patent/CH357722A/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Hydrogenated Pyridines (AREA)

Description

  

  



  Verfahren zur Herstellung eines neuen Hydrazin-Derivates
Es wurde gefunden, dass man zum neuen co- (l  Methyl-piperidyl-4)- (o-n-caproyl-hydrazin    gelangen kann, indem man   (l-Methyl-piperidyl-4)-hydrazin    mit Aceton umsetzt, das entstandene   oo-(l-Methyl-piperi-       dyl-4)-'-isopropyliden-hydrazin mit n-Capronsäure-    chlorid'acyliert und aus dem so entstandenen   co- (l-    Methyl-piperidyl-4)-?-n-caproyl-?'-isopropyliden-hydrazin die Isopropylidengruppe abspaltet.



   Beispiel    G    (1-Methyl-piperidyl-4)-?-n-caproyl-hydrazin    100 g (1-Methyl-piperidyl-4)-hydrazin    werden in 300 cm3 Aceton unter Kühlung gelöst und die Lösung   1/2    Stunde am Rückfluss zum Sieden erhitzt. Eindampfen der Lösung im Vakuum liefert das   co-(l-    Methyl - piperidyl - 4) -?' - isopropyliden - hydrazin in quantitativer Ausbeute. Es kristallisiert beim Abkühlen in Nadeln. Das Rohprodukt wird nicht weiter gereinigt, sondern gleich acyliert.



   Die Lösung von 18, 73 g   oo-(l-Methyl-piperidyl-      4)-co'-isopropyliden-hydrazin    in 100 cm3 Methylenchlorid wird unter Rühren und Kühlung mit einer Lösung von 14, 88   g      n-Capronsäurechlorid    in 25 cm3 Methylenchlorid versetzt. Nach beendeter Zugabe wird das Gemisch 4 Stunden bei Zimmertemperatur weitergerührt, dann mit 20proz., auf-10  abgekühlter, mit Kochsalz gesättigter   NatronTauge    ausgeschüttelt, über Natriumsulfat getrocknet und im Vakuum eingedampft.

   Der Rückstand wird im Hochvakuum fraktioniert, wobei das ? -(1-Methyl-piperidyl-4)-?-n  caproyl-o,'-isopropyliden-hydrazin    unter 0, 03 mm Hg bei 128-133   bergeht
20, 44 g   (,)-    (1-Methyl-piperidyl-4)-?-n-caproyl-?'isopropyliden-hydrazin werden in 100 cm3 90proz.



  ¯thanol gelöst und in die Lösung unter Eiskühlung Chlorwasserstoff eingeleitet bis zur stark sauren Reaktion auf Kongopapier. Nach einstündigem Stehen bei Zimmertemperatur wird die Lösung im Vakuum bei 12 mm Hg und bei einer Badtemperatur von 40 bis 50  fast zur Trockne eingedampft, der Rückstand in Methylenchlorid aufgenommen, die   Methylenchlo-      rid-Lösung    mit 20proz.,   auf-10     abgekühlter, mit Kochsalz gesättigter Natronlauge ausgeschüttelt, über Natriumsulfat getrocknet und im Vakuum eingedampft. Der kristalline Rückstand, das ?-(1-Methyl  piperidyl-4)-oo-n-caproyl-hydrazin,    wird aus Ather Petroläther umkristallisiert. Verwachsene Nadeln, Smp.   84-85 .     



   PATENTANSPRUCH
Verfahren zur Herstellung von ?-(1-Methyl-pipe  ridyl-4)-co-n-caproyl-hydrazin,    dadurch gekennzeichnet, dass man   (l-Methyl-piperidyl-4)-hydrazin    mit Aceton umsetzt, das entstandene   co- (l-Methyl-piperi-    dyl-4)-?'-isopropyliden-hydrazin mit   n-Capronsäure-    chlorid acyliert und aus dem so entstandenen   M- (l-       Methyl-piperidyl-4)-co-n-caproyl-cu -isopropyliden-hy-    drazin die Isopropylidengruppe abspaltet. 

**WARNUNG** Ende DESC Feld konnte Anfang CLMS uberlappen**.





  



  Process for the preparation of a new hydrazine derivative
It has been found that the new co- (l-methyl-piperidyl-4) - (on-caproyl-hydrazine) can be obtained by reacting (l-methyl-piperidyl-4) -hydrazine with acetone, the oo- ( l-methyl-piperidyl-4) -'- isopropylidene-hydrazine with n-caproic acid chloride'acylated and from the co- (l-methyl-piperidyl-4) -? - n-caproyl -? '- isopropylidene hydrazine splits off the isopropylidene group.



   Example G (1-methyl-piperidyl-4) -? - n-caproyl-hydrazine 100 g (1-methyl-piperidyl-4) -hydrazine are dissolved in 300 cm3 of acetone with cooling and the solution is refluxed for 1/2 hour Boiling heated. Evaporation of the solution in vacuo yields the co- (l-methyl-piperidyl-4) -? ' - isopropylidene - hydrazine in quantitative yield. It crystallizes in needles on cooling. The crude product is not purified any further, but acylated straight away.



   The solution of 18.73 g of oo- (l-methylpiperidyl-4) -co'-isopropylidene hydrazine in 100 cm3 of methylene chloride is mixed with a solution of 14.88 g of n-caproic acid chloride in 25 cm3 of methylene chloride while stirring and cooling . When the addition is complete, the mixture is stirred for a further 4 hours at room temperature, then extracted with 20% sodium hydroxide solution cooled to 10 and saturated with sodium chloride, dried over sodium sulfate and evaporated in vacuo.

   The residue is fractionated in a high vacuum, whereby the? - (1-Methyl-piperidyl-4) -? - n caproyl-o, '- isopropylidene hydrazine goes below 0.03 mm Hg at 128-133
20.44 g of (,) - (1-methyl-piperidyl-4) -? - n-caproyl -? 'Isopropylidene hydrazine are 90% in 100 cm3.



  ¯thanol dissolved and hydrogen chloride passed into the solution while cooling with ice until a strongly acidic reaction on Congo paper. After standing for one hour at room temperature, the solution is evaporated to almost dryness in vacuo at 12 mm Hg and a bath temperature of 40 to 50, the residue is taken up in methylene chloride, and the methylene chloride solution is 20%, cooled to -10, with sodium chloride Shaken out saturated sodium hydroxide solution, dried over sodium sulfate and evaporated in vacuo. The crystalline residue, the? - (1-methyl piperidyl-4) -oo-n-caproylhydrazine, is recrystallized from ether, petroleum ether. Intergrown needles, m.p. 84-85.



   PATENT CLAIM
Process for the production of? - (1-Methyl-pipe ridyl-4) -co-n-caproyl-hydrazine, characterized in that (l-methyl-piperidyl-4) -hydrazine is reacted with acetone, the co- ( 1-methyl-piperidyl-4) -? '- isopropylidene-hydrazine acylated with n-caproic acid chloride and from the M- (1-methyl-piperidyl-4) -co-n-caproyl-cu -isopropylidene -hydrazine splits off the isopropylidene group.

** WARNING ** End of DESC field could overlap beginning of CLMS **.



 

Claims (1)

**WARNUNG** Anfang CLMS Feld konnte Ende DESC uberlappen **. ** WARNING ** Beginning of CLMS field could overlap end of DESC **. Verfahren zur Herstellung eines neuen Hydrazin-Derivates Es wurde gefunden, dass man zum neuen co- (l Methyl-piperidyl-4)- (o-n-caproyl-hydrazin gelangen kann, indem man (l-Methyl-piperidyl-4)-hydrazin mit Aceton umsetzt, das entstandene oo-(l-Methyl-piperi- dyl-4)-'-isopropyliden-hydrazin mit n-Capronsäure- chlorid'acyliert und aus dem so entstandenen co- (l- Methyl-piperidyl-4)-?-n-caproyl-?'-isopropyliden-hydrazin die Isopropylidengruppe abspaltet. Process for the preparation of a new hydrazine derivative It has been found that the new co- (l-methyl-piperidyl-4) - (on-caproyl-hydrazine) can be obtained by reacting (l-methyl-piperidyl-4) -hydrazine with acetone, the oo- ( l-methyl-piperidyl-4) -'- isopropylidene-hydrazine with n-caproic acid chloride'acylated and from the co- (l-methyl-piperidyl-4) -? - n-caproyl -? '- isopropylidene hydrazine splits off the isopropylidene group. Beispiel G (1-Methyl-piperidyl-4)-?-n-caproyl-hydrazin 100 g (1-Methyl-piperidyl-4)-hydrazin werden in 300 cm3 Aceton unter Kühlung gelöst und die Lösung 1/2 Stunde am Rückfluss zum Sieden erhitzt. Eindampfen der Lösung im Vakuum liefert das co-(l- Methyl - piperidyl - 4) -?' - isopropyliden - hydrazin in quantitativer Ausbeute. Es kristallisiert beim Abkühlen in Nadeln. Das Rohprodukt wird nicht weiter gereinigt, sondern gleich acyliert. Example G (1-methyl-piperidyl-4) -? - n-caproyl-hydrazine 100 g (1-methyl-piperidyl-4) -hydrazine are dissolved in 300 cm3 of acetone with cooling and the solution is refluxed for 1/2 hour Boiling heated. Evaporation of the solution in vacuo yields the co- (l-methyl-piperidyl-4) -? ' - isopropylidene - hydrazine in quantitative yield. It crystallizes in needles on cooling. The crude product is not purified any further, but acylated straight away. Die Lösung von 18, 73 g oo-(l-Methyl-piperidyl- 4)-co'-isopropyliden-hydrazin in 100 cm3 Methylenchlorid wird unter Rühren und Kühlung mit einer Lösung von 14, 88 g n-Capronsäurechlorid in 25 cm3 Methylenchlorid versetzt. Nach beendeter Zugabe wird das Gemisch 4 Stunden bei Zimmertemperatur weitergerührt, dann mit 20proz., auf-10 abgekühlter, mit Kochsalz gesättigter NatronTauge ausgeschüttelt, über Natriumsulfat getrocknet und im Vakuum eingedampft. The solution of 18.73 g of oo- (l-methylpiperidyl-4) -co'-isopropylidene hydrazine in 100 cm3 of methylene chloride is mixed with a solution of 14.88 g of n-caproic acid chloride in 25 cm3 of methylene chloride while stirring and cooling . When the addition is complete, the mixture is stirred for a further 4 hours at room temperature, then extracted with 20% sodium hydroxide solution cooled to 10 and saturated with sodium chloride, dried over sodium sulfate and evaporated in vacuo. Der Rückstand wird im Hochvakuum fraktioniert, wobei das ? -(1-Methyl-piperidyl-4)-?-n caproyl-o,'-isopropyliden-hydrazin unter 0, 03 mm Hg bei 128-133 bergeht 20, 44 g (,)- (1-Methyl-piperidyl-4)-?-n-caproyl-?'isopropyliden-hydrazin werden in 100 cm3 90proz. The residue is fractionated in a high vacuum, whereby the? - (1-Methyl-piperidyl-4) -? - n caproyl-o, '- isopropylidene hydrazine goes below 0.03 mm Hg at 128-133 20.44 g of (,) - (1-methyl-piperidyl-4) -? - n-caproyl -? 'Isopropylidene hydrazine are 90% in 100 cm3. ¯thanol gelöst und in die Lösung unter Eiskühlung Chlorwasserstoff eingeleitet bis zur stark sauren Reaktion auf Kongopapier. Nach einstündigem Stehen bei Zimmertemperatur wird die Lösung im Vakuum bei 12 mm Hg und bei einer Badtemperatur von 40 bis 50 fast zur Trockne eingedampft, der Rückstand in Methylenchlorid aufgenommen, die Methylenchlo- rid-Lösung mit 20proz., auf-10 abgekühlter, mit Kochsalz gesättigter Natronlauge ausgeschüttelt, über Natriumsulfat getrocknet und im Vakuum eingedampft. Der kristalline Rückstand, das ?-(1-Methyl piperidyl-4)-oo-n-caproyl-hydrazin, wird aus Ather Petroläther umkristallisiert. Verwachsene Nadeln, Smp. 84-85 . ¯thanol dissolved and hydrogen chloride passed into the solution while cooling with ice until a strongly acidic reaction on Congo paper. After standing for one hour at room temperature, the solution is evaporated to almost dryness in vacuo at 12 mm Hg and a bath temperature of 40 to 50, the residue is taken up in methylene chloride, and the methylene chloride solution is 20%, cooled to -10, with sodium chloride Shaken out saturated sodium hydroxide solution, dried over sodium sulfate and evaporated in vacuo. The crystalline residue, the? - (1-methyl piperidyl-4) -oo-n-caproylhydrazine, is recrystallized from ether, petroleum ether. Intergrown needles, m.p. 84-85. PATENTANSPRUCH Verfahren zur Herstellung von ?-(1-Methyl-pipe ridyl-4)-co-n-caproyl-hydrazin, dadurch gekennzeichnet, dass man (l-Methyl-piperidyl-4)-hydrazin mit Aceton umsetzt, das entstandene co- (l-Methyl-piperi- dyl-4)-?'-isopropyliden-hydrazin mit n-Capronsäure- chlorid acyliert und aus dem so entstandenen M- (l- Methyl-piperidyl-4)-co-n-caproyl-cu -isopropyliden-hy- drazin die Isopropylidengruppe abspaltet. PATENT CLAIM Process for the production of? - (1-Methyl-pipe ridyl-4) -co-n-caproyl-hydrazine, characterized in that (l-methyl-piperidyl-4) -hydrazine is reacted with acetone, the co- ( 1-methyl-piperidyl-4) -? '- isopropylidene-hydrazine acylated with n-caproic acid chloride and from the M- (1-methyl-piperidyl-4) -co-n-caproyl-cu -isopropylidene -hydrazine splits off the isopropylidene group.
CH357722D 1958-05-06 1958-05-06 Process for the preparation of a new hydrazine derivative CH357722A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH354441T 1958-05-06
CH357722T 1958-05-06

Publications (1)

Publication Number Publication Date
CH357722A true CH357722A (en) 1961-10-31

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CH357722D CH357722A (en) 1958-05-06 1958-05-06 Process for the preparation of a new hydrazine derivative

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CH (1) CH357722A (en)

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