PURPOSE: To provide a new compound having testosterone-5α-reductase inhibition activity and as pharmaceutical for preventing androgen excess irritation or reducing its symptom, and used for remedy of such as benign prostatic hypertrophy, vulgaris acne, seborrhea, female rough hair.
CONSTITUTION: The compound (salt) of formula II is produced by allowing 17β-(carbomethoxy)-4-aza-5α-androstane-3-one expressed with formula I to react with dehydrogenation agent such as benzeoneselenic acid anhydride, forming double bond and hydrolyzing 17-carbomethoxy substituent, and after thioesterifying obtained steroid acid, to react with the Grignard reagent which prepared from 4-bromo-N,N-diethylaniline, etc., and then alkylating 4-aza nitrogen by need. In the formula II, R is H, methyl, ethyl; R2 is protectable phenyl substituted with N(R3) (R3 is a 1-4 alkyl, etc.); dotted line is double bond.
GIYARII ETSUCHI RASUMUSON
TOMASU ENU ZARUTSUMAN
