| 摘要 |
<p>PURPOSE:To provide a new indole derivative useful for the treatment and prevention of testosterone-alpha-reductase-relating diseases such as alopecia and prostatism. CONSTITUTION:The compound of formula I [R<1> is carboxy or protected carboxy; R<2> is H, lower alkyl or halogen; R<3> is aryl, ar(lower)alkyl, etc.; A is lower alkylene or lower alkenylene for oxo-substitution; Q is carbonyl or lower alkylene; X is group of formula II (R<4> is H or lower alkyl; R<5> is H, lower alkyl, etc.); Y is lower alkylene; Z is lower alkylene, -O-, etc.], e.g. 4-[3-[3-[bis(4- isobutylphenyl)methylamino]-benzoyl]indol-1-yl]butyric acid. The compound can be produced by reacting a compound of formula III [Z' is O or group of formula IV (R<6>a is H, lower alkyl, etc.)] with a compound of formula W<1>-R<3>a (R<3>a is ar(lower)alkyl, etc.; W' is acid residue) in a solvent (e.g. methanol) in the presence of a base (e.g. NaOH).</p> |
