| 摘要 |
<p>1,264,527. 2 - Guanyl - 1,2,3,4 - tetrahydrophthalazines. ORGANON LABORATORIES Ltd. 12 June, 1969 [23 July, 1968], No. 29766/69. Heading C2C. The invention comprises compounds of formula and their addition salts with therapeutically acceptable acids, wherein R 1 , R 2 , R 3 and R 4 are each H or C 1-4 alkyl, R 5 is H, C 1-6 alkyl, aryl or aralkyl, and X, Y are each H, OH, SH, C 1-6 alkoxy, halogen, NH 2 , CF 3 or SO 2 NH 2 . These compounds are prepared by reacting a compound of formula with (a) R 2 R 3 NCN or C 1-6 -alkyl-X-C(:NR 1 )- NR 2 R 3 where X = O or S, or their acid addition salts; (b) a 2-alkyl-1-nitroiso(thio)urea, followed by reduction of the 2-nitroguanyltetrahydrophthalazine so formed; (c) HSCN or alkyl-NCS to give a 2 - thiocarbamyltetrahydrophthalazine which is reacted with alkyl halide to give a 2-(1- alkylthio - 1 - imino)-methyltetrahydrophthalazine which in turn is reacted with R 2 R 3 NH. Exemplified starting materials, the preparation of which is described, are 2-benzyloxycarbonyltetrahydrophthalazine and 2-methyltetrahydrophthalazine. Therapeutic compositions for oral, parenteral or rectal administration comprise compounds of the above formula, which show antihypertensive activity.</p> |
