Document Type and Number:
Japanese Patent JPS5224017
Kind Code:
B1
Abstract:
1,258,023. A-Homo-steroids. CIBA-GEIGY A.G. 27 Jan., 1970 [30 Jan., 1969; 22 Dec., 1969], No. 3926/70. Heading C2C. Novel A-homo-steroids of the formula (wherein R 1 is a free or ketalized oxo group, or a #-positioned free, esterified or etherified hydroxy group together with a C 1-5 aliphatic hydrocarbon radical ; and R 2 is NH 2 or a free, esterified or etherified hydroxy group), and salts of the amino compounds, are prepared by reaction of the corresponding 3-unsubstituted- A-homo-steroids with hydrazine or with hydroxylamine or an ether or ester thereof. A 3- amino product may be converted to a 3-ol by reaction with a strong base, and the opposite conversion may be achieved with ammonia. 17- Ketals and esters and ethers may be hydrolysed and 17-ones may be converted to 17α-hydrocarbon - 17# - ols' by standard procedures. Free ols may be esterified and etherified. 4 - Methoxy - 3 - oxo - 17α - ethynyl - 17#- hydroxy - A - homo - #1,4,5(10) - - 19 - nor - androstatriene and the corresponding 17-ethylene ketal 'are formed as well as the expected 3-methoxy- 4 - oxo - #1(10),2,4a - 19 - nor - androstatrienes when the corresponding 3-ols are etherified with diazomethane. The A-homo-steroids of the invention are stated to possess estrogenic, antigonadotropic and spermicidal activity, and they may be made up into pharmaceutical compositions with suitable carriers.
Application Number:
JP805770A
Publication Date:
June 28, 1977
Filing Date:
January 30, 1970
Export Citation:
International Classes:
A61K31/12; A61P25/04; C07J63/00; C07J75/00; (IPC1-7): C07J63/00