CS231563B1 - Process for preparing steroid hormones with pregnane skeleton - Google Patents

Description

1

Pep, M? 45363

CnOCQB nOJiy EHMfl CTEPOM ^ ^ C HHX ΓΟΡΜΟΗΟΒ ΠΡΕΓΗΑΗΟΒΗΜ CKEJIETOM M3o6peTeHwe KacaeTcs cnocoóa nojiyneHMa cTeponflHBix γορμοηοβC NPE ΓΗ SHOBBIM ΟΚβΛΘΤΟΜ CO CBOÓ OflHHMH MJXM 3 aiqMipeHHHM5I ΓΗ # -ροκ CMJIbHHMM rpynnaMM, flaíOiqMMH BOSMOKHOCTb προ Μ 3B O £ b XT PEH-Hbie $ apMapeBTMnecKi IE ropMOKBi: Γπρ; ροκορτπ3θΗ, npep; 3WHonoH, 6-ΜΘΤΜΠΠρβρ; ΗΗ3ΟΛΟΗ X T.fl. M3BecTHa 3aiqwTa KapóoHMjibHon rpynnti KOJibpe b A b BWP e-BHM MHHOBOM COJI, KOTOpas ΠΟΟΠΘ ÓpOMPipOBaHXíI Μ CXE-amino-oBaTeoib ηογο aiíMTiumpoBaHMíi npeBpaiqaeTCH βρθτοκοη 3-21 17-γηγπ; ροκοπ nperHa-4-eH-3,20-flwoH / "PanxmaííHcyócTaHpnH - S -21-APET" / 0Θ3 ΑβφΜΗΗρΟΒΘΗΗΟΜ WTOTK HpOflyKTa ΠρΗ BbIXOfle 79% / 1, 2 / on Πρη KxaccMnecKOM cnocoóe nojiyneHMs cTepow £ Hsrx γορμοηοβ msflXO 3ΓΘΗΜΗΟΒΟ ΓΟ CBipbH nepBOHanax bHBIK npOflyKT COaepHHT ripppo KcwxbHyiO rpynny b-3 ~ θμ πολοηθκππ, KOTopan saipnipaeTcn APET-JlbHOM rpynnOM ΑΠΗ ΠρΟΒΘΑΘΗΗΗ COOTBST CTBymiIpíX peaKpMH C & yHK -iiíioHHpoBaHHfl b óokobom yrnepopíHon penx MoxeKyxu c penbiononyneHMH "PanxipanHcyócTaKnnM S 3 Otom cxynae npppoKcnjibHasrpynna pjoxscHa óbitb rn ^ ponorsosaHa π OKHcneHa 50 KapóoHTuibHOMrpynnbi b TeneHxe οτ, π, θλβηομ MHKpoÓJ / iajibHOM cTaj ^ wn, and caMoΓΜΙζρΟKCMJIWpOB ΒΗΜΘ B 1Ϊ-ΟΜ ΠΟΛΟΙΘΗΗίϊ Π ρΟΒΟ, ^ ΗΤ C?, BO BTOpOMMMKpOČIiaJIbHOM CTajtHM,

He, n; ocTaTKOM θτογο cnocoóa ηβληθτοη to, hto. npaKTxqecKwno ^ ynaeTíOfi cMecb yew hbvx θηημηηοββιχ cojrew, Ōjin 113 κοτορκχΟΙΜθΘΤ peaKpHOHHO cno COĎHy © flBOXHyíO CBH3b KOJIbpe B B M 2 cjisflOB8τθλbho ηθcta6wji3Ha NPW nocje ^ ysoiUMX onepapMHX, npOBOflMMLIX B SOKOBOM yTJiepOflHOM ΠΒΠΜ. 3aflaHeii M3o6peTeHMH ηβληθτοη co3;; aHHe cnocoóa nonyneHMaCTepowflHHX ropMOHOB c πρθΓΗθΗθΒΗΜ οκθλθτομ npw ynpomeH-hom θεηοοοeom κnananaeeom εhnaeeeom εnanaeeeckom pe;

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Cnocoó ocymecTBJíHeTCH rivet 3aiqwTH KapóoHWJiBHow rpynnub TpeTbeM nojioaceHMH b MoneKyne CTepow £ Horo cnejisTa, KOTopan conpaKeHa c ππομηομ cbh3bk) npwneM nowynaeTcneflMHCTBeHHLIM ΤθφΜΗΜΌΟΒ 8ΗΗΪ> Ι M npoyyKT, GTaÓOtHBM npMnoueíyaw peaKiíwnx b óokobow yrnepo £ HOK nenw m saipiiTtiΓΜ ^ ροκοΜΜΒΗΟΜ rpynnsr b 17-ow πο3ηηη? b b MoneKyne, npwneMnonynaeTcn npoayKT, γολκβιχ flnn MWKpoówanbHow oópaóoTKM3 CTepOHflHHW TOpMOH. 3

Cnocoó, corjiacHo n3oópeTeKiw, nojiynaeTCH θημμχηοββη CONHCO ΚΟΗΙΟΓΟΒ aHHOÍÍ CPICTeiíOM 513 C = NMC = G flBOÍÍHHX CBHSeH CT aÓMJIbHBIX ΠρίΙ 3ΛΘΚΤροφΜΛ bHMX peSKpMflX H 3aiqMTa ΓΧβρΟΚ CMJIh-HOM rpynnBI B 17-OX ΠΟ3ΜΙΤΜΜ O CymeCTBJIHeT CH rivet apeTKUIl / IPO BaHMH of Πρη ycjioBwjix nojiyneraa θημμηηοβομ conn wa enaMiiHa, onw-caHHbix 3 pMTMpoBaHHOfí nxTepaType, b npoflyxTe ocTamaMOJieKyjíK c ^ bomhlimh cbh3imim b κολxoee B 'coTieXo. B wHájpaKpacHOM cneKTpe nonynaeMoro npoayKTa what ^ ep-OKMTCH ΠΜΚ flBOMHOM CBH3M ΠρΜ 1610 CM COO Τ3ΘΤ CTByXWIMC = C £ BOMHOK CBH3H, COnpHXeHHOÍÍ CC = S JIBOMHOM CBíl3bíO, Μ ΠΜΚ NPW 1655 CM KOTOpHM COOTBeTCTByeT Η30 «ΊΜρ0Β aHHOÍÍ.0 = C flBOMHOÍÍ CBH3b £> (cm. CXBMy 1 /, IIOCJiBJíHEX ΠΜΚ HBJIH-θτοη noflTBepacfleHMeM npwcyTCTBKíi MOJiexyn c íibomhkmíí CBE-3HMH b KOJIblíe b ΠθρΘΜΘΐρθΗΜΘ 3T0M ^ BOMHOíÍ CBH3M b ΚΟΛ &amp; ΠΟA socTMraeTca rivet noflanw cncTeMe αοποληχτθλβηοχ sHeprnn, npnneM nojiyxíaeTCíi what ^ b what ^ epacaipaH tojibko oahh πμκ ííbom HHX-CBSSeH ΠΟΜ 1610 CM Te nOMyneHHKM NPO ^ yXT COíepjKMTtojibko KOHioroBaHHyíO cxcTeMy W3 C m N = C = 0 jtbomhhx οβη3θμ.3to ri; oKa3aHo taxxi οπθκτροΜ HMP. nojiyneHHan cnocoóoM corjiacHo Μ3θδρβτβΗΜ2) cojib očecnennsaeTκολμμθοτβθηηοθ npoTeKamie nocjieflyioinMx peaKiíMM - ópoMnpo-BaHMH Μ ΤΜΛΚςθΤΜΛΚρΟΒΘΗΜΗ. 330ρΟΜΗΟΘ ΠρΟM 330flEC θ ojcojim / 21-6poM-17-rMApoKCKnperHa-4-oH-3,20-xhoh / corjiacHoΜ30όρβτβΗΜκ? Ϊ́Μβθτ τ. nji, 219-220 ° 0 Torna, kbk of njza-BjreHMa co about cTsyioipe for 3όομηογο προμ3βορ; για cynn nonaTeHTy ΦΡΓ 1,801,410-165 ° C, μρομμή TpanctiopMMe-βTTiTiHP-PanTiPiTiPaTiPiTiPiTiPiTiPiTiPiTiPiTiPiTiPe / 21-ΤρθΤθκοη-17-Γηηροκοίΐ-πρβΓΗ3-4-ΘΗ-3,20-hxoh / n 4 οδρ86sthb8θτch apeTWjiwpvKiiemem cMecbft ajis 3 8µmth rn, npoKcwjibn h3i wpyu hpyi rpy; ΠοοΛθΛΗβθ ocymecTBjíHeTCfí npwnoMomw AU eTMjxwpyiomeM cMecw W3 yKcycHoro aHrwpjpwjTa b-pac TBopMTejie c κβτθλμτμηθοκομ CMEC &amp; io xnopHaa KwcjiOTa b θτμλβ-LíeTaTe, npwneM weSeraeTCH ynoTpeóweHwe floporocTonmeroTpw $ TopyKcycHoro aHrwflpwaa, ynoTpeSxaeMoro b πολο6ηβιχ CNY-qaax. Ycjiobhh noíioSpaHH tskmm oópa3OM, Anette ητο MpoBaHwerwflpoKcwjibHOH rpynnbi ^ b-17 ow no3Mu; ww npoTexaeT κολμπθοτβθη-HO 6θ3 Η3ΜΘ ΗΘΗΜίϊ θθ ΟΤΘΧΗΟΜΘΤρΜΗ and K ap6OIIWJI ΒΗ8Η rpynna b TpeTBex πο3ηπμμ b cTepoíiflHOM cKexeTe MOJiexywbi ocTasTcncBočoflHon mjih npeBpamaeTCH eHowaiieTaT b. Ποολθλημη ηθβ, μηθτ npoBe Ha, and; eHxe MMKpoówajibHoS CTA ^ o-11- -rwflpoKcw jixpoBaHHH, Tax κax b ycwoBMnx ero προβθ ^ OH θημη cpaeyrx / w ípojiHsyeTCH ocsoSoac ^ AET KapSoHHWbHyro rpynny, canpn aceHHyK-c abočíhoíí οβηθβκ. JDnOCOČ, eorxaCHO Μ3θ6ρβΤΘΗΗΚ) ^ ΛΗ 3aiIíHTbI B 17-om ΠΟΛΟτΚΘΗΗΗ -OH rpynnil npWCyTCTBMH KapÓOHHWbHOH rpyniIK B B-3 ΘΜ ΠΟΛΟ -aceHMM ^ AET βο3μοοκηοοτβ npoBOAWTb γηλροκοηλμροβθηηθ b-17 omΠΟΛΟΚΘΗΗΜ rivet OflHOKpaTHOH MMKpOĎΜ3ΛbHOM OÓpaČOTKM.

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Q xaGíyreHHOMy cyxoMy MeTaHOxosoMy pacTBopy / 15 - 20 0/3

XXOpHOX KXCXOTbl / 500 CM paCTBO OCTSEjlíIST £ 0 ΠρΧΟδρθΤΘΗΚΗ ΚΟΜΜΤΗΟΜθΜΠβρθΤρ'ρΒΙν pa36a3XHK> T xočaBoxHKM κοχχηθοτβομ cyxoro MeTanoxa 3 3 250 CM M pe y KO KO KO KO KO KO KO KO KO KO Ocayox nepxjiopaTHOK οολη pacocopneTCH, npxxeM pacTsop ocscpBe ^ PiBaeTCH. nocxe oxxaac-O 3 3θηηη 30 30 - 33 C KaruiHMM npxĎaBXHiOT 2 cm SpoMa, pacT-ΗΗΟΓΌρθΗΗΟΓΌ B 50 CM3 CyXOTO MeTaHOJia. 3θ3 W3OJIWpOBaHMíI ÓpOM-Ρ ΠΡ0Μ3Β03Η0Γ0 33ΙΙΐ; py rpynna y CTpaHHST ca np W Ó aBJíeH 20120 cm3 HgO m 10 r KgCOg, npeflBapHTeJibHO p30T3opeHf. npw 9T0M mejio ^ Hooí oópaSoTKe MaTepxaxa, kotophhnpoBOflMTca b θ θ n aca n nx 30 ° C Taxation nponycxaeT cTpyxa3OTa. PjiaBHoe χοχμμθοτβο cnxpTa oTflecTxxxpyeTCH NPW Baxa-YME / TeMnepaTypa κμπθημη 30-35 ° C / x nojiyneHKLiM ocTaTOXpaaóati Fletch ^ 50 to 60 ^ xpaTHHM kojuímsctbom χολο ηομ boijh.IIojiyxaeTCH SexEix OCA / ζοχ W3 21-6poM 17-rnflpoxcM nperHa-4- ΘΗ-3,20-flHOHa, ΧΟΤΟρΗΧ φΗΧΒΤργΒΤ, npOMLTBasOT OOBOBHOχολο, τ; ηομ βολομ n cymaT b cTpye τθπλογο -50 ° C. 210-215 ° C pacTBOpnioT B500 cm ° aireTOHa, R 5 co.yepac.aiyero aqeTaTa xaxwíi n pacTsopΧΜΠΗΤΧΤ NPW OÓpaTKOM XOJIOBMJIBHHXe B ΤΘΜΘΗΜθ 2-3 qacOB onocjie oTflecTMxupoBaHXH ochobhoto aojixnecTBa aiíSTOHapa3ÓaBJIÍíK) T 50-60 XpaTHLIM KOJIWCTBOM JTE n; HHOM SOflH MnpoyyxT φχχΒτργκτ pi npoMHBaiOT bool. noxyxeHHyio PaxxmaíÍH cyScTaHiíMso-S-21-APET cyuiaT μ χχπήτητ C 4-5 xpaTHSiMxojixnecTBOM MeTaHOJia, pa3ÓaBJiHKiT čojibuizm KoawcraoM bump oxxaacyaioT p o 0 μ φχχΒτργιοτ «BucyinenHLiM 21 au; eToxcx-17-RW /]; poKCM -nperHa-4-eH-3,20- [m.p.] to 240 ° C.

Bbixoy 9 rpaMMOB. 10 r PaxxuXH-cyocTaHiyM- S -21-apeTaT pacTBopasT with 20 cm3MeTHJ1HXJiopHfla, ± 0 cm yxcycHoro aHrxflpxya w 10 cm xaTa-xxTxnecxox cMecx K3 sTiexe3; OmsCB 3βΚΚΠ3ΘΤχ nojiyqaeTCB pacTsop. ´4epea 3-4 Maca au.eTxxxpoBaHiie oxohmsho x Τ3ΗΠΗ £

noxynaeTCi cMecb-5- 17,21-yxaireT M3 yB.yx nofofVKTOB - PaKxmaMH-cyOC-aT x PaxxqaxH-cylo CTaKiMH-S-3,17,21, -TpxapsTaT. Ilocxe οχλβικ, π, θηηη pacTBopa .yo. 30 ΠρΧδθΒΧΒΙΌΤ 100 cm3 weTaHOJia. 3 npwcyTCTBww useTasoja w kwcjiobo xaTa-ww3aTopa οβοΘορηημ yKcycHHw aHrMflpwp nepeocTepwábwpwpyeTcs3 QTMjiapeTaT b Teweswe 3-4 wacos NPW κομηβτηομ TeMnepa-Type- PacTBopwTSJíB OTnecTwnwpyeTCíí £ 0 nojiyweHHH rycTOííKpMCTaKímecKOH Cain κοτορβη pasSaBnaeTca so.pow w nonywa-iotcíi Seaiae KpwcTajuiii οοοτβθτ cTByi cipwx-2- apeTaTHHX npow3Bon-hsix PaííxmaMH cyocTaHiínx-S npwweM OCA co.pepacaT samw-ipeHKyzo apeTM.ziO3i.iM papwKanoM rwppoKcwwBHyio rpynny b-17 omnojioaceHMM «Ποολθ Φμλβτροβηηκη w 3ηο; / κιμβ3ηηη KpwcTajrzwqecKOMáčen nojiywaiOT οκολο 10 r npopyKTa, ropworo PWN MWKpoówajibΗΟΓΟ rWppOKCMWWpOBaHMa b 11 -OM nOJIOaCeHHM. 10

ΦΟΡΜΟΑ M30BPETEHW

CnOCOÓ ΠΟΛγ ^ ίθΗΜΗ ΟΤβρΟΙίρΗΗΧ ΓΟρΜΟΗΟΒ C ΠΌΘ ΓΗ ΒΗΟΒΗΜ ΟΚΘΛΘ-τομ πγτθΜ 3ampiTbi KapĎOHJObHOíl rpynna β τρθτβθμ πολο, τκθηχμB ΜΟΛΒΚγΛβ CTSpOMflHOrO 0ΚβΛΘΤ3 3 BHfle eHMMIIHOBO 1 COJI, ČpOMWpOBaHUH, ΓΗ £ ρθΛΜ38 33ΐρΐΙΤΗ0Η ΓργΠΠΗ Β © Μ ΠΟΛΟΟΚΘΗΗΚ 3, 21 β-aiíeTsumpoBaHHfl ομ πολοχθηκη, sanyiTH πί ^ ροκοοόκοζ rpyn-ΠΗ Β 17 ΟΜ ΠΟΛΟΚΘΗΜίί Μ ΜΗΚρΟδΐΊΟΛΜΟΓΌ ΓΙί £ ρθ Κ C ΠΛΜρ038ΗΙΙΗ 'Β 11 ΟΜ ΠΟΛΟΟΚΘΗΙΙΜ, ΟΤΙΓΠΗδΙΌΙΟ, ΙίίϊΰΠ ΤΘΜ5 ΠΤΌ ΘΗΗΜΙίΗ Ο ΟΒΧΠΒΙΟΤπρΜ ΗΗ3Κ0Η TeMnepaType to κμολογο pacTSopa x noxyHeHHyiooněch cojieii neperpyímpyioT nyTew HarpeBaHiiH with ο .ρηο3Η3τπηοfle $ MHíipOBaHHyiO BHXMIIHOSyiO COJIb C 0 £ ΜίΜ eppíHCTBSHHblM MKOíCOnpSXeHHHX pBOIHHXIX 03Η3θΗ ΚΚ ρφρβΚρθΟΗΟΜ ΘΚΤΠΘΚΤρeroo ΌΜΠΘΚΤρθo MwpoBaHxe x nippojiiis 3anyiTHoxrpynnbí β 3 θμ 'nojioxeoii προΒορ, πτ b: ES-ρθβκγγκοηηομ as Cyperus 3 am,WTa ΓχρροκοιυίΒΗΟκ rpynnu 17 β-om ιμοηθηο NPO-sopyiTCH rivet ayeTMJiMpoBaHMíi yKcycHHM aarx piiflOM ^ w: kmcjiomKaTajiM3aTope npx Haxiiniíii οβοοοληοχ KapČoHíuibHoii rpynnaΒ 3 -βΜ ΠΟΛΟΚΘΗΧΧ ζΘΤΜΛ ζΘΤΜΛ ζΘΤΜΛ HO r Β Β Β Β--η η η η η η η η η η η η η η η η η

AHHOTAIW Κ Μ 30 6ρ βΤ e ΗΙΊΚ "Cnocoč nOJiy ^ EHW CTepOM £ HbIX POpMOHOBC Πρθ ΓΉ &amp; ΗΟΒΒΙΜ ΟΚΘΛΘΤΟΜ" Μθοδρθτθκκθ KacaeTCH cnocoóa nonyneHna cTepon / íHHX ropMOHoac nperaaHoshiM cnejieTOM what cboóoahkmm mjih 3 3πιρΕΐθΗΗϊ> ΐΜΗ γηρ; -pOKďUIbHHMH rpynnSMM, ^ aiOIpMMX 303M0SCH0CTL · H3P0T0BHSTb ΙτθΗ-HBie $ apMatresTi-mecKMe ropMonti: mnpoxopTH3OHnpe £ hm3ojioh, 6-MeTMX-npeflHr.130JI0H Η T.fl. 3ajTaneíí w3oSpeTeHi-ia ηβληθτοη co3flaHne cnocoóa nonynsannCTepOUflHHX ΓΟρΜΟΗΟΒ C Πρβ ΓΗΗΗΟΒΒΙΜ ΠρΜ ynOOipeH-hom τθχηολο me ckom peacMMB wTBeCeNNeNTeNeNTeNeNTeNeNTeNeNNe.

GnocoÓo conacHO nsoSpeTeHMsa, 4jih nonynsHna cTepoz ^ HsrxropMOHOB c nperaaHOBbíM CKejieooM rivet 3aurnTbi xapóoHrab-hom rpynnhí b 3 θμ nonoaceHwn b Monexyne cTepon ^ Horo cxeneTaB BK ^ e ΘΗΜΜΗΗΟΒΟίί COJIW COCTOHT 3 TOM ΗΤΟ ΘΗ3ΗΜ O CaKflaiOTπρη HM3K0M TeMnspaType n3 kmchopo pacTBOpa m nonyneHHyio cMecbcojiew neperpynwpy®T rivet HarpesasHn b oflKosnanKo ρβφηΗη-pOBaHHyiO eHTlMMHOByiO COJIb C OnHMM eíMHCT3eKHbIM ΠΚΚ0Μ conpfí-SCBHHKX ηΒΟΜΗΗΧ 0ΒΗ3ΘΜ b $ MH paKpaCHO.M ΟΠΘΚΤΡΘ ΠΟΗ 1610 01.1--1 night-nero προΒοηητ ópOMnpoBaHne n m.nponns 33ίΐριτκοη rpynnsrb 3-EIM Nonoh b tom ne ρβοκρηοπηοΜ cocy ^ e. 3aipnTa nmpo-KCíiJibHOÍÍ rpynnbi b 17-om πολοϊθηκε ocym, ecT3jiHeTCH nyTenapeTiuíMposaHna yKcycHHM aHmnpwyroM κ kiicjiom 'KaTanneaTopenpn Hannnwn cbočouhoh KapóoHHJibHOn rpynnsi and 3-θμ πολοηθηοm apeTMJibHoří rpynnbi b 21-om nojioneHwn n nop; BepraeTCH ο, ρηοκ-path MnxpoóManbHon oópaóoTKe jijih rnypoKciumpoBaHiiH with 11-omnonoiaeHMH.

Claims (1)

SUMMARY OF THE INVENTION Process for the preparation of steroid hormones with pregnane skeletal blocking of the carbonyl group at the 3-position in the steroid skeleton in the form of the enimine salt, by thawing, byprolysis of the 3-position acetylation at the 21 position, protecting the hydroxyl group at the 17 position and the microbial hydroxylo characterized in that the enamine is precipitated at a temperature of 10 to 15 ° C from the acidic solution and the resulting mixture of salts is rearranged at the boiling point in methanol to the enimine salt with a single peak of conjugated double bonds in the infrared spectrum at 1 610 cm -1, then wherein the reaction vessel is subjected to thawing and hydrolysis of the 3-position protecting group, protecting the hydroxyl group at position 17 by acetylation with acetic anhydride and an acid catalyst in the presence of the free 3-carbonyl group &amp; the acetyl group at position 21, whereupon the product obtained is subjected to microbial hydroxylation at position 11. Recognized by the invention based on the results of an expert study carried out by the Institute for Inventions and Innovations, Sofia, BG i