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71. 发明专利

EA008411B1 СПОСОБ СИНТЕЗА ВЫСОКОЧИСТОГО ОКСИМА D-(17α)-13-ЭТИЛ-17-ГИДРОКСИ-18,19-ДИНОРПРЕГН-4-ЕН-20-ИН-3-ОНА 未知
公开(公告)号：EA008411B1
公开(公告)日：2007-04-27
申请号：EA200600119
申请日：2004-04-29
申请人： RICHTER GEDEON VEGYESZET
发明人： TUBA ZOLTAN , MAHO SANDOR , KISS JANOS , MAGYARI ENDRENE , TERDY LASZLO
IPC分类号： C07J41/00 , C07J1/00
摘要： Изобретениеотноситсяк способусинтезавысокочистогооксима d-(17α)-13-этил-17-гидрокси-18,19-динорпрегн-4-ен-20-ин-3-она (далее - норэлгестромина) путемацетилирования d-норгестрелав положении 17, оксимированияоксогруппыв положении 3 полученного 17-ацетоксипроизводногои, взаключение, гидролизаацетоксигруппыв положении 17 полученного 3-оксимногопроизводного. Способподанномуизобретениюсостоитв следующем: исходноевещество d-(17α)- 17-гидрокси-13-этил-18,19-динорпрегн-4-ен-20-ин-3-он (d-норгестрел), чистота 93-94%, ацетилируютуксуснымангидридомв уксуснойкислотев присутствиихлоридацинкаи хлороводородаили 70% перхлорнойкислотыв атмосфереинертногогаза, ипослезавершенияреакцииизбытокуксусногоангидридаи побочныйпродукт "енолацетат" разлагаютсолянойкислотой, затемполученный d-(17α)-17-ацетокси-13-этил-18,19-динорпрегн-4-ен-20-ин-3-онвыделяютизреакционнойсмеси, добавляясмесьводысольдом, выпавшийв осадокпродуктотфильтровывают, промываютводой, сушат, растворяютв дихлорметанеилиацетоне, ирастворосветляютсиликагелемилиоксидомалюминияи активированнымуглем, послеотфильтровыванияосветлителяполученныйрастворконцентрируют, иостатокперекристаллизовывают, полученный d-(l7α)-17-ацетокси-13-этил-18,19-динорпрегн-4-ен-20-ин-3-онвводятвовзаимодействиеилис ацетатомгидроксиламмония, илис хлоридомгидроксиламмонияв присутствииацетатанатрияв уксуснойкислотев атмосфереазотаприэнергичномперемешиваниив течениепримерно 1 ч, послезавершенияреакциидобавляютводу, выпавшийв осадокпродуктотфильтровывают, промываютводой, сушати перекристаллизовывают, полученныйоксим d-(17α)-17-ацетокси-13-этил-18,19-динорпрегн-4-ен-20-ин-3-онагидролизуютэквивалентнымколичеством

73. 发明专利

CA2528952A1 PROCESS FOR THE SYNTHESIS OF HIGH PURITY D-(17ALPHA)-13-ETHYL-17HYDROXY-18,19-DINORPRE:GN-4-ENE-20-YNE-3-ONE-OXIME 未知
公开(公告)号：CA2528952A1
公开(公告)日：2005-01-06
申请号：CA2528952
申请日：2004-04-29
申请人： RICHTER GEDEON VEGYESZET
发明人： TERDY LASZLO , TUBA ZOLTAN , MAHO SANDOR , KISS JANOS , MAGYARI ENDRENE
IPC分类号： C07J41/00 , C07J1/00
摘要： The invention relates to a process for the synthesis of high purity d- (17.alpha.)-13-ethyl-17~hydroxy-18,19-dinorpregn-4-ene-20-yne-3-one-oxime (further on norelgestromine) via acetylation of d-norgestrel at position 17, oximation of the oxo group at position 3 of the obtained 17-acetoxy derivative, and finally hydrolyzing the acetoxy group at position 17 of the obtained 3-oxime derivative. The process according to our invention is as follows: the starting material, d-(17.alpha.-17-hydroxy-13-ethyl-18,19- dinorpregn-4-ene-20-yne-3~one (d-norgestrel) - purity 93-94 % - is acetylate d with acetic anhydride in acetic acid, in the presence of zinc chloride and hydrogen chloride, or 70 % perchloric acid in an inert gas atmosphere, and after completion of the reaction the excess of acetic anhydride and the "eno l acetate" by-product are decomposed with aqueous hydrochioric acid, then the formed d-(17.alpha.)-17-acetoxy-13-ethyl-18,19-dinorpregn-4-ene-20-yne-3-one is isolated from the reaction mixture by addition of ice-water, the precipitated product is filtered off, washed with water, dried, dissolved in dichloromethane or acetone and clarified with silica gel or aluminum oxide a nd charcoal, after filtration of the clarifier the resulted solution is concentrated and the residue is recrystallized,the obtained d-(17.alpha.)-17 - acetoxy-13-ethyl-18,19-dinorpregn-4-ene-20-yne-3-one is reacted either with hydroxylammonium acetate or with hydroxylammonium chloride in the presence o f sodium acetate, in acetic acid in nitrogen atmosphere under vigorous stirrin g for about 1 hour, after completion of the reaction water is added, the precipitated product is filtered off, washed with water, dried and recrystallized, the obtained d-(17.alpha.-17-acetoxy-13-ethyl-18,19-dinorpre gn- 4-ene-20-yne-3-one-oxime is hydrolyzed with an equivalent amount of an alkal i metal hydroxide in a C1-C4 alkanol solution, in nitrogen atmosphere between a temperature of about 5-38 ~C, under vigorous stirring, after completion of t he reaction the mixture is diluted with water and the pH of the resulted suspension is adjusted to 7,5-9 with acetic acid, the precipitated product i s filtered off, washed with water, dried, the crude product is dissolved in ethanol, clarified with charcoal, and after filtration of the clarifier wate r is added to the obtained solution, the precipitated high purity d-(17.alpha. )- 17-acetoxy-13-ethyl-18,19-dinorpregn-4-ene-20-yne-3-one-oxime is filtered of f, washed with water and in given case recrystallized from ethanol.

74. 发明专利

HU9901939A2 PROCESS FOR PRODUCING A-NOR-SECO-STEROIDE COMPOUNDS, SECO-INDOXYLIDENECARBOXILICACID DERIVETIVES AS INTERMEDIATES THEREOF 未知
公开(公告)号：HU9901939A2
公开(公告)日：2001-03-28
申请号：HU9901939
申请日：1999-06-10
申请人： RICHTER GEDEON VEGYESZET
发明人： SANTA CSABA , MAHO SANDOR , TUBA ZOLTAN , SZILAGYI GABRIELLA , BAKCSI ERIKA , SZELES JANOS , BALOGH GABOR , BRLIK JANOS , TRISCHLER FERENC DR
IPC分类号： C07C51/285 , C07D209/36 , C07C62/06
摘要： The invention relates to a new process for the synthesis of 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-3-acid derivatives of formula (I)wherein the meaning of Z is carboxyl or formyl group andto the new secoindoxylidene carboxylic acid derivatives of formula (II)wherein R1 and R2 independently are C1-C4 alkyl or alkoxy group, hydrogen or halogen atom-which are intermediates for preparing the compounds of formula (I).The 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-3-acid derivatives of formula (I) are intermediates in the synthesis of oxandrolon (17beta-hydroxy-17alpha-methyl-2-oxa-5alpha-androstane-3-one), which is used as anabolic in therapy.

75. 发明专利

HU9901938A2 NEW PROCESS FOR PRODUCING 17-BETHA-HYDROXY-17-ALPHA-METHYL-2-OXA-5-ALPHA-ANDROSTAN-3-ON, AS WELL AS INTERMEDIATE THEREOF 未知
公开(公告)号：HU9901938A2
公开(公告)日：2001-03-28
申请号：HU9901938
申请日：1999-06-10
申请人： RICHTER GEDEON VEGYESZET
发明人： SANTA CSABA , MAHO SANDOR , TUBA ZOLTAN DR , MESTER TAMAS , TROMPLER ARPAD , SZELES JANOS , LANCOS KRISZTINA DR , FODOR KATALIN FERENCZINE DR , HORVATH PETER DR
IPC分类号： C07J73/00 , C07J75/00
摘要： The invention relates to a new process for the synthesis of 17beta-hydroxy-17alpha-methyl-2-oxa-5alpha-androstane-3-one of formula (I). The process according to the invention is as follows: the 17beta-hydroxy-17alpha-ethyl-1,3-seco-2-nor-5alpha-androstane-1,3-diacid of formula (III) is transformed into the ring-closed 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-1,3-diacid anhydride of formula (II) in an inert solvent or without solvent with a C2-C3 alkan acid anhydride or a substituted carbodiimide of formula R1-N=C=N-R2- wherein R1 and R2 independently are C1-C6 alkyl group, C1-C6 alkyl group substituted by tertiary or quaternary amino group or 1-3 phenyl group, C5-C6 cycloalkyl group, aryl group substituted by 1-3 methoxy, tertiary amino, nitro, C1-C4 alkyl group or 1-3 halogen atom-and the obtained compound of formula (II) is reduced regioselectively by a complex alkali metal hydride in an inert solvent The new 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-1,3-diacid anhydride of formula (II) is also the subject of the invention.

76. 发明专利

AU5239600A New process for the synthesis of 17beta-hydroxy-17alpha-methyl-2-oxa-5alpha-androstane-3-one 未知
公开(公告)号：AU5239600A
公开(公告)日：2001-01-02
申请号：AU5239600
申请日：2000-05-26
申请人： RICHTER GEDEON VEGYESZET
发明人： SANTA CSABA , TUBA ZOLTAN DR , MAHO SANDOR , SZELES JANOS , FERENCZI KATALIN , HORVATH PETER , LANCOS KRISZTINA , MESTER TAMAS , TROMPLER ARPAD
IPC分类号： C07J73/00 , C07J75/00
摘要： The invention relates to a new process for the synthesis of 17beta-hydroxy-17alpha-methyl-2-oxa-5alpha-androstane-3-one of formula (I). The process according to the invention is as follows: the 17beta-hydroxy-17alpha-ethyl-1,3-seco-2-nor-5alpha-androstane-1,3-diacid of formula (III) is transformed into the ring-closed 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-1,3-diacid anhydride of formula (II) in an inert solvent or without solvent with a C2-C3 alkan acid anhydride or a substituted carbodiimide of formula R1-N=C=N-R2- wherein R1 and R2 independently are C1-C6 alkyl group, C1-C6 alkyl group substituted by tertiary or quaternary amino group or 1-3 phenyl group, C5-C6 cycloalkyl group, aryl group substituted by 1-3 methoxy, tertiary amino, nitro, C1-C4 alkyl group or 1-3 halogen atom-and the obtained compound of formula (II) is reduced regioselectively by a complex alkali metal hydride in an inert solvent The new 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-1,3-diacid anhydride of formula (II) is also the subject of the invention.

80. 发明专利

NO944749A 未知
公开(公告)号：NO944749A
公开(公告)日：1995-02-08
申请号：NO944749
申请日：1994-12-08
申请人： RICHTER GEDEON VEGYESZET
发明人： MAHO SANDOR , TUBA ZOLTAN , GERE ANIKO , VITTAY PAL , KISS BELA , PALOSI EVA , SZPORNY LASZLO , CZINEGE ERZSEBET FRANCSICSNE , BOORNE ANNA MEZEI , BALOGH GABOR , GOROG SANDOR
IPC分类号： A61K31/57 , A61K31/58 , A61P3/06 , C07D239/42 , C07D239/48 , C07D239/50 , C07D491/10 , C07J20060101 , C07J9/00 , C07J43/00
CPC分类号： C07D239/42 , C07D239/48 , C07D239/50 , C07D491/10 , C07J43/003

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