PURPOSE: To provide a new compound that prevents and reduces the sign of androgen overstimulation as testosterone reductase inhibitor, and is used for treatment of acne, seborrhea and female rough hair locally, and of benign prostatic hypertrophy in generally.
CONSTITUTION: The compound and its salt or ester expressed by formula II is produced by allowing 17β-(carbomethoxy)-4-aza-5α-androstane-3-one to react with dehydrogenation agent of benzene selenic acid anhydride, to form double bond, then to hydrolyze the obtained 17-carbomethoxy substituent into steroid acid, to be esterified, and then to alkylate 4-aza-nitrogen with Grignard reagent, if need. In the formula II, R is H, methyl, ethyl; R2 is (protection)hydroxy, O1-4C alkyl, 1-4C alkyl, formula (CH2)mOH ((m) is 1-4), formula (CH2)nCOOH ((n) is 1-3), dotted line is double bond which can exist.
GIYARII ETSUCHI RASUMUSON
TOMASU ENU ZARUTSUMAN
