| 摘要 |
1501236 8 - Alkyl - 7 - phenyl - pyrido[3,4-d]- pyridazines TAKEDA YAKUHIN KOGYO KK 27 March 1975 [28 March 1974] 12901/75 Heading C2C Novel compounds and their salts (in which R 1 is C 1-2 alkyl and R 2 is a 5- or 6- membered cyclic amino group containing one or more N-atoms and optionally substituted by at least one C 1-4 alkyl group) are prepared by reacting a compound II in which X is halogen, with an amine R 2 H and, if desired, recovering the compound in the form of a salt. Compounds I (R 1 =Me, R 2 =morpholino, 2-methyl morpholino; R 1 =Et, R 2 = morpholino, piperidino) are prepared. Compounds II (X=C1) are prepared by a Diels-Alder reaction between 4-phenyl-5-(R 1 )- oxazole and N-phenylmaleimide to give 3,N- diphenyl - 4 - (R 1 ) - 7 - oxa - 2 - aza - bicyclo- (2,2,1) - hept - 2 - ene - 5,6 - dicarboxamide which is reacted with cone. HCl to form 2,N-diphenyl- 3 - (R 1 ) - pyridine - 4,5 - dicarboxamide which is reacted with hydrazine hydrate in glacial acetic acid to give 7-phenyl-8-(R 1 )-1,2,3,4-tetrahydropyrido[3,4-d]pyridazine-1,4-dione which is halogenated with POCl 3 . Compounds I are diuretics and form wth a carrier or diluent a pharmaceutical composition which may be administered orally or parenterallv. |
