专利号:US-5438134-A 优先权日:1990-07-09 标 题:Process for the production of unsaturated 17 α-cyanomethyl-17 β-h 发明人:TEICHMUELLER GERHARD; MUELLER GERD 权利人:JENAPHARM GMBH 摘要:The unsaturated 17α-cyanomethyl-17β-hydroxy steroids of the formula I, ##STR1## in which R 1 =Me, Eth; R 2 =H, Me; R 3 =H, OH, an acetoxy or alkoxy group; R 4 =H, R 5 =OH, an acetoxy, alkoxy group of R 4 and R 5 together represent a keto- or ketal group and double bonds are contained in the basic structure of the steroid, particularly between the 15 and 16 position in the steroid ring, from unsaturated 17-ketosteroids of the general formula II as described herein with the aforementioned meanings of R 1 to R 5 by reacting the unsaturated 17-ketosteroids with LiCH 2 CN and subsequently hydrolyzing. n The compounds of formula I are pharmacologically interesting steroid compounds or also intermediate products for the synthesis of highly-effective steroid products which can be used in human and veterinary medicine for the treatment of endocrine disorders and for reproductive control based on their specific hormonal/anti-hormonal actions. n The compounds are suitable for the treatment of endometriosis and also in combination with preparations with ethinylestradiol for fertility control.
参考标题:Process For The Production Of Unsaturated 17 .Alpha.-Cyanomethyl-17 .Beta.- 摘要:The Unsaturated 17.Alpha.-Cyanomethyl-17.Beta.-Hydroxy Steroids Of The Formula I, ##str1## In Which R.Sub.1 =me, Eth; R.Sub.2 =h, Me; R.Sub.3 =h, Oh, An Acetoxy Or Alkoxy Group; R.Sub.4 =h, R.Sub.5 =oh, An Acetoxy, Alkoxy Group Of R.Sub.4 And R.Sub.5 Together Represent A Keto- Or Ketal Group And Double Bonds Are Contained In The Basic Structure Of The Steroid, Particularly Between The 15 And 16 Position In The Steroid Ring, From Unsaturated 17-Ketosteroids Of The General Formula Ii As Described Herein With The Aforementioned Meanings Of R.Sub.1 To R.Sub.5 By Reacting The Unsaturated 17-Ketosteroids With Lich.Sub.2 Cn And Subsequently Hydrolyzing. The Compounds Of Formula I Are Pharmacologically Interesting Steroid Compounds Or Also Intermediate Products For The Synthesis Of Highly-Effective Steroid Products Which Can Be Used In Human And Veterinary Medicine For The Treatment Of Endocrine Disorders And For Reproductive Control Based On Their Specific Hormonal/anti-Hormonal Actions. The Compounds Are Suitable For The Treatment Of Endometriosis And Also In Combination With Preparations With Ethinylestradiol For Fertility Control.