| 摘要 |
NEW MATERIAL:The 2-substituted amino-4(1H)-pyrimidone derivative of formula I (R<1> is alkyl; R<2> is H or lower alkyl; m and n are 1-3) or its salt. EXAMPLE:2-{2-{{{2-[(Diaminomethylene)amino]-4-thiazolyl}methyl}thio}-e thyl amino}6-methyl-5-propyl-4(1H)-primidone. USE:Pharmaceuticals. It has histamine H2-receptor antagonistic activity and gastric mucosa protecting action, and is useful as a remedy for gastropathy, e.g. an agent to suppress the such as gastric acid secretion, remedy for gastric ulcer, etc., having low side effect. PREPARATION:The compound of formula I can be prepared e.g. by reacting the amine of formula II with 2-nitroamino-4(1H)-pyrimidone derivative of formula III in the absence of a solvent at a high temperature, or in an inert organic solvent under heat-refluxing, if necessary in the presence of a reaction accelerator such as pyridine, etc. |
