Preparation of triazolo [1, 5-c] pyrimidines as potential antiasthma agents

…, R Paul, JS Baker, JA Brockman, MT Du…

文献索引：Medwid, Jeffrey B.; Paul, Rolf; Baker, Jannie S.; Brockman, John A.; Du, Mila T.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 4 p. 1230 - 1241

全文：HTML全文

被引用次数: 129

摘要

With the use of the human basophil histamine release assay, 5-aryl-2-amino [1, 2, 4] triazolo [1, 5-c] pyrimidines were found to be active as mediator release inhibitors. These compounds were prepared by reacting arylamidines with sodium ethyl formylacetate or with ethyl propiolate to give pyrimidinones. Treatment with phosphorus oxychloride gave a chloropyrimidme, which was converted to a hydrazinopyrimidine with hydrazine. ...