发明授权
US4550100A Process for the preparation of 17.alpha.-bromoethynyl- and
17.alpha.-iodoethynyl-17.beta.-hydroxy steroids and novel products
thereof
失效
制备17α-溴乙炔基 - 和17α-碘代乙炔基-ββ-羟基类固醇的方法及其新产物
- 专利标题： Process for the preparation of 17.alpha.-bromoethynyl- and 17.alpha.-iodoethynyl-17.beta.-hydroxy steroids and novel products thereof
- 专利标题（中）： 制备17α-溴乙炔基 - 和17α-碘代乙炔基-ββ-羟基类固醇的方法及其新产物
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申请号： US552537申请日： 1983-11-16
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公开(公告)号： US4550100A公开(公告)日： 1985-10-29
- 发明人: Helmut Hofmeister , Paul E. Schulze , Klaus Annen , Henry Laurent , Rudolf Wiechert
- 申请人： Helmut Hofmeister , Paul E. Schulze , Klaus Annen , Henry Laurent , Rudolf Wiechert
- 申请人地址： DEX Berlin and Bergkamen
- 专利权人： Schering Aktiengesellschaft
- 当前专利权人： Schering Aktiengesellschaft
- 当前专利权人地址： DEX Berlin and Bergkamen
- 优先权： DEX3242892 19821116
- 主分类号： G01N33/53
- IPC分类号： G01N33/53 ; A61K51/00 ; A61K51/04 ; C07J1/00 ; C07J63/00 ; A61K31/56
摘要：
A process for preparing bromine- or iodine-unlabeled or radioactively labeled 17.alpha.-bromoethynyl- and 17.alpha.-iodoethynyl-17.beta.-hydroxy steroids of the androstane and estrane series of the partial formula ##STR1## wherein is a single bond or a double bond,V is a carbon-carbon bond or a methylene group,R is hydrogen or methyl, andX is bromine or iodine,from corresponding 17.alpha.-ethynyl-17.beta.-hydroxy steroids, comprises treating the starting steroid in an inert solvent with a brominating agent or an iodinating agent in the presence of a silver salt.The process enables production of old and new compounds having value as pharmacologically active compounds and also as diagnostic agents when the iodine or bromine is radioactive.