PURPOSE: To obtain the subject compound useful as an intermediate for a 5α-reductase inhibitor in excellent yield by reacting an amide compound with a halogen or its equivalent in the presence of an alcohol and a base and then carrying out the dealkoxycarbonylation, etc.
CONSTITUTION: This method for producing a 1-substituted phenyl-1-alkylamine derivative expressed by formula III (R1a, R1b and R1c each is H or a 1-6C alkoxy; R2 and R3 each is a 1-6C alkyl, with the proviso that R1a to R1c are not simultaneously H) is to react an amide compound expressed by formula I with a halogen or its equivalent in the presence of an alcohol expressed by the formula R4OH (R4 is a 1-6C alkyl or a 7-14C aralkyl) and a base, provide a compound expressed by formula II and then carry out the dealkoxycarbonylation of the prepared compound expressed by formula II. The resultant compound expressed by formula III is useful as an intermediate for producing azasteroids having excellent inhibiting actions on 5α-reductases. Compounds expressed by formula IV, etc., are cited as the azasteroids which are useful for benign prostatic hypertrophy, acne, seborrhea, female hypertrichosis, male baldness, prostatic cancer, etc.
KURATA HITOSHI
ISHIBASHI KIMIKI
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