PURPOSE: To obtain the subject new steroid derivative useful as a bisosynthesis inhibitor of esterogens, a therapeutic agent for diseases such as mammary cancer, uterine cancer, etc., caused by excessive estrogen, etc., having a specific molecular structure and excellent aromatase inhibitory action.
CONSTITUTION: A mixture of methyltriphenylphosphonium bromide and ethyl ether is mixed with 15% solution of n-butyl lithium in n-hexane and stirred in a nitrogen flow at room temperature for 30 minutes. The mixture is blended with a mixture of a D-homo-17-oxaandrosta-4-ene-3,17a-dione, etc., and a diethyl ether, stirred at room temperature for 5 minutes, then the reaction mixture is blended with 10% hydrochloric acid and the extract is purified by thin layer chromatography to give the objective steroid derivative useful as a therapeutic agent of the formula (R1 is H, halogen, lower alkyl, etc.; R2 and R3 are H or lower alkyl; A is C=O or CH2; B is O or NH; (n) is 1 or 2) useful for mammary cancer, uterine cancer and having excellent aromatase inhibitory action.
TAKEGAWA YOSHIHIRO
IWASHITA SHIGEKI
KAWACHI TOMOKO
HONMA SEIJIRO
TAKAHASHI HIROO
SAEGUSA MAMORU
MINATO KOICHI
SHIBATA TAKEO
