| 摘要 |
PROBLEM TO BE SOLVED: To obtain an indole derivative useful as a therapeutic agent for prostatic hypertrophy, prostatic cancer, baldness and acne, having inhibitory action on steroid 5α-reductase. SOLUTION: This indole derivative (salt) is shown by formula I R<1> is H or CHR<3> R<4> [R<3> and R<4> are each H, a lower alkyl or a (substituted) aryl]; R<2> is a group of formula II or III (R<5> and R<6> are each H or a lower alkyl)} such as 4-[2-(indol-5-yl)-1H-4-quinolinone-8-oxy]butyric acid. The derivative, for example, is obtained by condensing an indolecarboxylic acid with aniline to give a compound of formula IV (R<9> is a lower alkyl; Ac is acetyl), reacting the compound in the presence of a base such as sodium methoxide in an organic solvent such as methanol, etc., at a room temperature to a temperature under reflux for 30 minutes to 6 hours and reacting the resultant substance in the presence of a base such as potassium t-butoxide, etc., in a solvent such as dimethylformamide, etc., at 0-50 deg.C for 30 minutes to 6 hours.
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