摘要 |
1318643 3 - Amino - 4 - halo - sydnonimine derivatives BOEHRINGER INGELHEIM GmbH 21 Aug 1970 [22 Aug 1969] 40477/70 Heading C2C Novel 3 - amino - 4 - halo - sydnonimine derivatives of the general formula wherein R 1 is a methyl group and R 2 is a methyl or α-methylbenzyl group, or R 1 and R 2 , together with the nitrogen atom to which they are attached, form a hexamethyleneimino, morpholino or N-methylpiperazino group, Hal is a chlorine, bromine or iodine atom and R 3 is an allyloxy, phenoxy or benzyloxy group or, when R 1 and R 2 , together with the nitrogen atom to which they are attached, form a morpholino group and Hal is a chlorine or bromine atom, a C 1-4 alkoxy group, and acid addition salts thereof are prepared by halogenation of a 3-amino-sydnonimine derivative of the general formula followed optionally by salification of the product. 3 - Amino - sydnonimine derivatives of the second general formula above are prepared by acylation of the corresponding 3-amino-sydnonimine with a chloroformate of the general formula ClCOR 3 . Pharmaceutical compositions having bloodpressure decreasing activity comprise, as active ingredient, a 3-amino-4-halo-sydnonimine derivative of the first general formula above or a physiologically acceptable acid addition salt thereof, in association with a pharmaceutical carrier or excipient, and may be administered enterally or parenterally. |