| 摘要 |
1,217,661. Hydrazino - benzocinnolines and benzocycloheptapyridazines. BRISTOLMYERS CO. 7 Jan., 1969 [11 Jan., 1968], No. 1033/69. Heading C2C. Novel compounds of the formula wherein X and Y are alike or different and each is H, F, Cl, Br, CF 3 , OH, C 1-6 alkyl, C 1-6 alkoxy, NH 2 or NO 2 ; and n is 1 or 2, or non-toxic, pharmaceutically acceptable acid addition salts thereof, are obtained by reacting a compound of the formula with an excess of hydrazine hydrate. The preparation of intermediates is described as follows:- 1 - Tetralone - 2 - acetic acid is refluxed with hydrazine hydrate to form 2,3,4,4a,5,6-hexahydro - 3 - oxo - benzo[h]cinnoline which is treated in glacial acetic acid with bromine to form 2,3,5,6 - tetrahydro - 3 - oxo - benzo[h] cinnoline and the latter is heated with POCl 3 to yield 5,6 - dihydro - 3 - chloro benzo[h]cinnoline. By similar methods starting from benzosuber-1- one-2-acetic acid there are obtained 2,3,4,4atetrahydro - 3 - oxo - benzocyclohepta[5,6-c] pyridazine, 2,3 - dihydro - 3 - oxobenzocyclohepta[5,6-c]pyridazine and 3-chlorobenzocyclohepta[5,6-c]pyridazine. α-Tetralone is reacted with bromoacetic acid to yield 1-tetralone-2- acetic acid. Pharmaceutical compositions having hypotensive action comprise a compound of Formula (1) above or a salt thereof as above and a pharmaceutical carrier in forms suitable for oral, parenteral or rectal administration. |
