发明授权
US3894004A Novel 11-oxygenated pregneno (17,16{60 -D)-1,3-oxathiolanes and process for the preparation thereof
失效
新型11-氧合孕烯（17,16（60-D）-1,3-氧硫杂环戊烷）及其制备方法
- 专利标题： Novel 11-oxygenated pregneno (17,16{60 -D)-1,3-oxathiolanes and process for the preparation thereof
- 专利标题（中）： 新型11-氧合孕烯（17,16（60-D）-1,3-氧硫杂环戊烷）及其制备方法
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申请号： US42660073申请日： 1973-12-20
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公开(公告)号： US3894004A公开(公告)日： 1975-07-08
- 发明人: HOFMEISTER HELMUT , LAURENT HENRY , PREZEWOWSKY KLAUS , WIECHERT RUDOLF , MENGEL KLAUS , WENDT HANS
- 申请人： SCHERING AG
- 专利权人： Bayer Schering Pharma AG
- 当前专利权人： Bayer Schering Pharma AG
- 优先权： DE2264001 1972-12-22
- 主分类号： C07J7/00
- IPC分类号： C07J7/00 ; C07J13/00 ; C07J31/00 ; C07J41/00 ; C07J71/00 ; C07C173/00
摘要：
Topical anti-inflamatory 11-oxygenated pregneno(17,16 Alpha -d)1'', 3''-oxathiolanes of the formula I
wherein R1 and R2, can be the same or different and are a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkyl containing hetero atoms, aryl, or heteroacyl; R1 and R2 together can be a (CH2)n bridge which can also contain hetero atoms, and wherein n has the values of 2-6; R3 represents a hydrogen or fluorine atom, or an alkyl; X is a hydrogen, fluorine, or chlorine atom; Y is an oxygen atom or the group
WHEREIN R4 represents a hydrogen atom or an acyl; and C1 .... C2 represents a single or double bond between the C-1 and C-2 carbon atoms. This invention also comprises the process of producing the compounds by condensation of 16 Beta -hydroxy-17 Alpha mercaptopregnenes with carbonyl compounds under epimerization of the substituent at the C-16 carbon atom.
wherein R1 and R2, can be the same or different and are a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkyl containing hetero atoms, aryl, or heteroacyl; R1 and R2 together can be a (CH2)n bridge which can also contain hetero atoms, and wherein n has the values of 2-6; R3 represents a hydrogen or fluorine atom, or an alkyl; X is a hydrogen, fluorine, or chlorine atom; Y is an oxygen atom or the group
WHEREIN R4 represents a hydrogen atom or an acyl; and C1 .... C2 represents a single or double bond between the C-1 and C-2 carbon atoms. This invention also comprises the process of producing the compounds by condensation of 16 Beta -hydroxy-17 Alpha mercaptopregnenes with carbonyl compounds under epimerization of the substituent at the C-16 carbon atom.