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    • 6. 发明授权
      EP0190759B1 11 Beta-Phenyl-Gonane, deren Herstellung und diese enthaltende pharmazeutische Präparate 失效
    • 11 Beta-Phenyl-Gonane, deren Herstellung und diese enthaltende pharmazeutische Präparate
    • EP0190759B1
    • 1989-08-30
    • EP86101548.5
    • 1986-02-06
    • SCHERING AKTIENGESELLSCHAFT
    • Neef, Günter, Dr. , Wiechert, Rudolf, Prof. , Ottow, Eckard, Dr. , Rohde, Ralph. Dr. , Beier, Sybille, Dr. , Elger, Walter, Dr. , Henderson, David, Dr.
    • C07J1/00 , C07J15/00 , C07J21/00 , C07J41/00 , C07J53/00 , A61K31/565 , A61K31/585 , C07J5/00 , C07J7/00
    • C07J1/0096 , C07D319/06 , C07J1/0081 , C07J15/00 , C07J21/003 , C07J21/006 , C07J41/0083 , C07J53/004
    • 1. Claims (for Contracting States : BE, CH, DE, FR, GB, IT, LU, NL, SE) 13-alkyl-11 beta-phenyl-gonanes of general formula I see diagramm : EP0190759,P23,F3 wherein A and B together represent an oxygen atom, a CH2 group or a second bond between carbon atoms 9 and 10, X represents an oxygen atom or the hydroxyimino grouping N apprch OH, R1 represents a straight-chained or branched, saturated or unsaturated hydrocarbon radical having up to 8 carbon atoms that is to contain the grouping see diagramm : EP0190759,P23,F4 with X having the meaning mentioned above, R2 represents a methyl or ethyl radical in the alpha- or beta-configuration, wherein, in the case of a methyl or ethyl radical in the alpha-configuration, R3 /R4 represents see diagramm : EP0190759,P23,F5 see diagramm : EP0190759,P24,F1 or see diagramm : EP0190759,P24,F2 and wherein, in the case of a methyl or ethyl radical R2 in the beta-configuration, R3 /R4 represents see diagramm : EP0190759,P24,F3 with R5 representing a hydrogen atom or an acyl radical having from 1 to 4 carbon atoms, Y representing a hydrogen, chlorine, fluorine, iodine or bromine atom, or an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group each having from 1 to 4 carbon atoms in the or each alkyl or acyl radical, R6 representing a hydrogen atom, a hydroxy group, or an alkyl, O-alkyl or O-acyl group each having from 1 to 4 carbon atoms, m representing 0, 1, 2 or 3, R7 representing a hydroxy or cyanide radical, or an O-alkyl or O-acyl group each having from 1 to 4 carbon atoms, and k representing 0, 1 or 2, R8 representing a hydrogen atom, or an alkyl or acyl group each having from 1 to 10 carbon atoms, R9 , R10 , R11 and R12 each represents a hydrogen atom, a hydroxy group, or an alkyl, alkoxy or acyloxy group each having from 1 to 4 carbon atoms, or a halogen atom, and the substituent of the 11 beta-phenyl radical is in the 3- or 4-position. 1. Claim (for Contracting State AT) Process for the manufacture of compounds of general formula I see diagramm : EP0190759,P26,F4 wherein A and B together represent an oxygen atom, a CH2 group or a second bond between carbon atoms 9 and 10, X represents an oxygen atom or the hydroxyimino grouping N apprch OH, R1 represents a straight-chained or branched, saturated or unsaturated hydrocarbon radical having up to 8 carbon atoms that is to contain the grouping see diagramm : EP0190759,P27,F1 with X having the meaning mentioned above, R2 represents a methyl or ethyl radical in the alpha- or beta-configuration, wherein, in the case of a methyl or ethyl radical in the alpha-configuration, R3 /R4 represents see diagramm : EP0190759,P27,F2 or see diagramm : EP0190759,P27,F3 and wherein, in the case of a methyl or ethyl radical R2 in the beta-configuration, R3 /R4 represents see diagramm : EP0190759,P27,F4 see diagramm : EP0190759,P28,F1 with R5 representing a hydrogen atom or an acyl radical having from 1 to 4 carbon atoms, Y representing a hydrogen, chlorine, fluorine, iodine or bromine atom, or an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group each having from 1 to 4 carbon atoms in the or each alkyl or acyl radical, R6 representing a hydrogen atom, a hydroxy group, or an alkyl, O-alkyl or O-acyl group each having from 1 to 4 carbon atoms, m representing 0, 1, 2 or 3, R7 representing a hydroxy or cyanide radical, or an O-alkyl or O-acyl group each having from 1 to 4 carbon atoms, and k representing 0, 1 or 2, R8 representing a hydrogen atom, or an alkyl or acyl group each having from 1 to 10 carbon atoms, R9 , R10 , R11 and R12 each represents a hydrogen atom, a hydroxy group, or an alkyl, alkoxy or acyloxy group each having from 1 to 4 carbon atoms, or a halogen atom, and the substituent of the 11 beta-phenyl radical is in the 3- or 4-position, characterised in that a compound of general formula II see diagramm : EP0190759,P28,F2 wherein K represents a blocked keto group in the form of a ketal, thioketal, oxime or methyloxime, A, B and R2 have the meanings mentioned above, R'1 has the same meaning as R1 but contains a see diagramm : EP0190759,P28,F3 instead of a see diagramm : EP0190759,P28,F4 grouping, R'3 has the same meaning as R3 , any hydroxy groups being protected, and R'4 has the same meaning as R4 , any hydroxy or acyl groups being protected, and K1 , in addition to having the meanings mentioned above for K, also represents a hydrogen atom and a protected hydroxy group, is subjected to the influence of a dehydrating agent that is also capable of freeing the protected function(s), in order to split off water while simultaneously forming the 4(5) double bond, a hydroxy group contained in K1 is oxidised, if desired the compounds of general formula I so obtained, with R9 , R10 , R11 and R12 representing one hydrogen atom each, are reacted by microbiological hydroxylation with microorganisms of the species Streptomyces toyocaensis (DSM 40030) and/or Streptomyces platensis (NRRL 2364) and/or Nigrospora sphaerica (CBS 98469) and/or Neurospora crassa (ATCC 9278), and, if desired, the hydroxylated compounds of general formula I so obtained, wherein at least one of the substituents R9 , R10 , R11 and R12 represents a hydroxy group and the remaining substituents represent hydrogen, are epimerised at the positions carrying the hydroxy groups, if desired the hydroxy groups are etherified, esterified or replaced by a halogen or alkyl radical, if desired the hydroxy groups present in R3 and R4 are esterified or etherified, to from the product of general formula I with X representing an oxygen atom and, if desired, reaction is subsequently carried out with hydroxylamine hydrochloride in the presence of tertiary amines at temperatures of between - 20 degrees C and + 40 degrees C.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明公开
      EP0051143A1 Verfahren zur Herstellung von 3-beta,7-beta-Dihydroxy-delta-5-steroiden 失效
    • Verfahren zur Herstellung von 3-beta,7-beta-Dihydroxy-delta-5-steroiden
    • 一种用于3-β，7-β-二羟基δ-5-类固醇的制备方法。
    • EP0051143A1
    • 1982-05-12
    • EP81107458.2
    • 1981-09-19
    • SCHERING AKTIENGESELLSCHAFT
    • Petzoldt, Karl, Dr. , Wiechert, Rudolf, Prof. , Laurent, Henry, Dr. , Nickisch, Klaus, Dr. , Bittler, Dieter
    • C12P33/06 , C07J53/00
    • C12P33/06 , C07J53/008 , C07J71/001
    • Ein Verfahren zur Herstellung von 3ß,7ß-Dihydroxy-Δ 5 - steroiden der allgemeinen Formel I
      worin Q die Gruppierungen
      und R, ein Wasserstoffatom, eine Trimethylacetylgruppe, eine tert.-Butyl-dimethylsilylgruppe, eine Dimethyl-2-(3-methylbutyll-silylgruppe oder eine Tribenzylsilylgruppe darstellen, welches dadurch gekennzeichnet ist, daß man ein 3ß-Hydroxy-Δ 5 -steroid der allgemeinen Formel II
      worin Q die obengenannte Bedeutung besitzt und R 2 ein Wasserstoffatom oder eine Alkanoylgruppe mit 2 bis 6 Kohlenstoffatomen darstellt, mit einer Kultur von Botryodiplodia malorum fermentiert, und gewünschtenfalls die erhaltenen 3ß,7ß-Dihydroxy-Δ 5 -steroide der allgemeinen Formel mit Trimethylacetanhydrid, tert-Butyl-dimethyl-silylchlorid, Dimethyl-2-(3-methyl-butyl)-silylchlorid oder Tribenzyisilylchlorid umsetzt.
    • 一种用于制备3β，过程7β二羟基Δ<5>通式I <图像>其中Q是分组和R1是氢原子，三甲基乙酰基，叔丁基二甲基甲硅烷基，二甲基 - 2 -steroids - （3-甲基丁基）甲硅烷基，或表示三苄基，其特征在于，一个3β羟基Δ<5>通式-steroid II 其中Q具有上述含义和R 2表示氢原子或 表示链烷酰基碳原子数为2〜6，发酵与Botryodiplodia malorum的培养物，并且如果需要的话，3β获得，7β二羟基Δ<5>通式I与三甲基乙酸酐的类固醇，叔丁基 - 二甲基 - 甲硅烷基氯，二甲基 2-（3-甲基 - 丁基）甲硅烷基氯或Tribenzylsilylchlorid反应。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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