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1. 发明授权

US3437657A 6-fluoromethyl-3-oxo-4,6-dienic steroids and process for preparing same 失效
标题翻译： 6-氟代-3-OXO-4,6二氧化物类固醇及其制备方法
公开(公告)号：US3437657A
公开(公告)日：1969-04-08
申请号：US3437657D
申请日：1965-12-17
申请人： BRITISH DRUG HOUSES LTD
发明人： ELLIS BERNARD , FEATHER PETER , MACBRIDE HUGH , PETROW VLADIMIR
IPC分类号： C07J1/00 , C07J5/00 , C07J71/00 , C07J75/00 , C07C169/30 , A61K17/00 , C07C169/34
CPC分类号： C07J71/00 , C07J1/00 , C07J5/00 , C07J75/00

2. 发明专利

GB1063921A 6-fluoromethyl-í¸ and í¸-3-oxo-steroids 未知
公开(公告)号：GB1063921A
公开(公告)日：1967-04-05
申请号：GB5194664
申请日：1964-12-21
申请人： BRITISH DRUG HOUSES LTD
发明人： ELLIS BERNARD , FEATHER PETER , MACBRIDE HUGH , PETROW VLADIMIR
IPC分类号： C07J1/00 , C07J5/00 , C07J71/00 , C07J75/00
摘要： 6 - Fluoromethyl - D 4,6 and D 1,4,6 - 3 - oxosteroids, some of which are novel, are prepared by treating 6 - hydroxymethyl - D 4,6 - 3 - oxosteroids with a fluorinating agent and, if desired, dehydrogenating. The preferred fluorinating agent is 2-chloro-1,1,2-trifluorotriethylamine. The steroids are preferably of the pregnane or androstane series or their 19-norderivatives and may contain in the 11-position a b -OH or keto group, in the 9-position a fluorine atom, in the 16-position =CH2, CH3, CN, CH2OH, a halogen, =CH.CH3 or =CHX or CH2X (wherein X is a halogen), in the 17-position the group b -COCH2R (wherein R is H, OH, O acyl or a halogen) with or without a 17a -R1 group (wherein R1 is OH, O acyl or alkyl) or a 16a ,17a -methylenedioxy group containing one or two alkyl or aryl groups or wherein the methylene group is part of a cycloalkyl ring, or in the 17b -position the group OH or O acyl. They may additionally contain D 9(11)- or D 16-double bonds. A large number of other optional substituents are also referred to, as described in Specification 1,030,885. 17a - Ethyl - 6 - hydroxymethyl - pregna - 4,6-diene-3,20-dione is prepared by reacting 17a -ethyl - 3 - methoxy - pregna - 3,5 - dien - 20-one with the Vilsmeier reagent to give 17a -ethyl - 6 - formyl - 3 - methoxy - pregna - 3,5-dien - 20 - one, reducing this to 17a - ethyl - 6-hydroxymethyl - 3 methoxypregna - 3,5 - dien-20 - one and reacting this with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone. Reference has been directed by the Comptroller to Specification 961,249.ALSO:Pharmaceutical compositions comprise 6-fluoromethyl-3-oxo-D 4,6 and D 1,4,6-steroids of the androstane, 19-nor-androstane, pregnane and 19-nor-pregnane series and carriers. They may also contain an estrogen, and may show a large variety of steroidal properties. Tablets containing 17a - acetoxy - 6 - fluoromethyl-16-methylenepregna-4,6-diene-3,20-dione and ethynylestradiol and an emulsified ointment containing 21-acetoxy-6-fluoromethyl-17a - hydroxy -pregna-4,6-diene-3,11,20-trione are described and other standard formulations are referred to.

3. 发明专利

CA802889A 6 FLUOROMETHYL-3-OXO-4,6-DIENIC STEROIDS OF THE ANDROSTANE OR 19-NORANDROSTANE SERIES 未知
公开(公告)号：CA802889A
公开(公告)日：1968-12-31
申请号：CA802889D
申请人： BRITISH DRUG HOUSES LTD
发明人： ELLIS BERNARD , FEATHER PETER , PETROW VLADIMIR , MACBRIDE HUGH

4. 发明专利

GB1070761A 6-fluoromethyl-í¸4,6-3-oxo-steroids 未知
公开(公告)号：GB1070761A
公开(公告)日：1967-06-01
申请号：GB2068665
申请日：1965-05-17
申请人： BRITISH DRUG HOUSES LTD
发明人： ELLIS BERNARD , FEATHER PETER , MACBRIDE HUGH , PETROW VLADIMIR
IPC分类号： C07J1/00 , C07J75/00
摘要： Novel steroids of the formula wherein R1 is hydrogen or methyl; R2 is fluorine chlorine, bromine, CF3, hydrogen or C1- 5-alkyl; and R3 is hydrogen, methyl or ethyl; are prepared by treating the corresponding 6-hydroxymethyl steroids with 2-chloro-1,1,2-trifluoro-triethylamine. 17a - Chloroethynyl - 6 - hydroxymethyl - 17b - methoxy - 19 - norandrosta - 4,6 - dien - 3 - one is prepared by reducing 17a -chloroethynyl-6-formyl 3,17b - dimethoxy - 19 - norandrosta - 3,5 - diene (prepared from the corresponding 6-unsubstituted-2,5(10)-diene, phosgene and dimethylformamide) with sodium borohydride to the corresponding 6-hydroxymethyl compound and treating this with 2,3-dichloro-5,6-dicyano-benzoquinone. The corresponding free 17b -ols are prepared similarly.

5. 发明专利

CA758582A 6-FLUOROMETHYL-3-OXO-.DELTA.4,6-STEROIDS 未知
公开(公告)号：CA758582A
公开(公告)日：1967-05-09
申请号：CA758582D
申请人： BRITISH DRUG HOUSES LTD
发明人： FEATHER PETER , ELLIS BERNARD , PETROW VLADIMIR , MACBRIDE HUGH

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