abstract |
1382916 3-(2-Piperazinoethyl)-indoline derivatives AMERICAN CYANAMID CO 3 May 1972 [27 May 1971] 20674/72 Heading C2C The invention comprises compounds of formula and their pharmacologically acceptable acid addition and quaternary ammonium salts, wherein R 1 is H, Cl, Br, C 1-4 alkoxy, NO 2 , NH 2 , MeCOHN or Me 2 N, and R 2 is H, C 1-4 alkoxy or NO 2 (or R 1 -R 2 may be -OCH 2 O-); R 3 and R 4 are each H or Me; and R 5 is H, Cl, MeO, Me or CF 3 . These compounds are prepared by (1) reducing the corresponding indole; (2) reacting a corresponding 1 - acyl - 3 - XCH 2 CH 2 - indo- line (where X is Cl, Br, MeSO 3 or p-TsO) with a 4-phenylpiperazine, and removing by hydrolysis the 1-acyl groups from the 1-acyl derivative of I thus formed. Also prepared is an intermediate of Formula I where R 1 = MeO, R 2 = NH 2 , R 3 = Me and R 4 = R 5 = H. |