process for the manufacture of 17alfa - ethynyl - (5alfa) - 2 - androsten - 17 - beta - the olympics.

摘要

1492746 #SP2/SP-Androstenes THERAMEX SA 17 Jan 1975 [17 Jan 1974] 02211/74 Heading C2U [Also in Division A5] The invention comprises 17-ethynyl-5- androst-2-en-17#-ol and its acetate free from their respective #SP3/SP-isomers; and their preparation from the analogously pure corresponding 17-one by reaction with an alkali metal salt (simple or complex) of acetylene, followed when required by acetylation. 5 - Androst - 2 - en - 17 - one is freed from admixed #SP3/SP-isomer thereof by treatment with Jones reagent and isolation of the pure #SP2/SP compound from the resultant mixture, e.g. by crystallization or chromatography. (The #SP3/SP- isomer is thought to be converted to a diacid or aldehyde while the #SP2/SP-isomer remains unchanged). The inventive compounds are credited with pituitary gonadotrophin-stimulating, gonadinhibiting, antitumour, contraceptive, anti-parathyroid and anti-seborrhoeic activities, and may be made up with carriers into pharmaceutical compositions for oral, parenteral, topical and rectal administration.