| 摘要 |
<p>(A) Indole derivs. (I) R1=H, halogen, OH, alkyl, alkoxy, NH2, alkyl/acylamino; R2,3=H, alkyl R4=H, halogen, NH2, OH, alkyl (B) Intermediates of formula (II), below (I) have anti-inflammatory and antipyretic props. (a) A mixture of N'-(p-methoxyphenyl)-N'-(p-chlorobenzoyl)hydrazine. HCl (3.2 g), 4-thio-phenone-2-carboxylic acid (2g) and AcOH (15 ml) is heated at 80 deg. for 3 hr. to give (N-(p-chloro-benzoyl)-5-methoxy)indole-2,3:3', 4'-(2'-carboxy)-dihydrothiophen, crystd. from t-BuOH. (b) This (3 g) is gently refluxed with a suspn. of Raney Ni (30 g) in EtOH (500 ml) for 4 hr. to give N-(p-chlorobenzoyl)-5-methoxy-2-methyl -3-indolyl acetic acid, m.p 151 deg. (t-BuOH).</p> |
