BGC-20-1178, RS-1178
Chemical Name: 5-Methyl-8-(1-phenylethyl)-7,8-dihydro-6H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-a]pyrimidine
CAS No. 62052-82-8
项目整合开发状态: Preclinical
项目研究机构: BTG (Proprietary), Sankyo (Originator)
合成路线:The cyclization of 1,2,4-triazol-5-amine (I) with 3-acetyltetrahydrofuran-2-one (II) by heating at 155 C gives the triazolopyrimidinone (III) (1),which is treated with refluxing POCl3 to yield 7-chloro-6-(2-chloroethyl)5-methyl-1,2,4-triazolo[1,5-a]pyrimidine (IV).Finally this compound is cyclized with 1-phenylethylamine (V) by means of Na2CO3 in refluxing ethanol to afford the target pyrrolo-triazolo-pyrimidine derivative.
📌 参考资料/链接：
参考文献标题:Pyrrolotriazolopyrimidine derivs.and process for the preparation thereof
文献作者:Takagi,H.; Sato,Y.; Shimoji,Y.; Kumakura,S.(Sankyo Co.,Ltd.)
参考来源:US 4007189
📄 详细内容
合成路线:The cyclization of 1,2,4-triazol-5-amine (I) with 3-acetyltetrahydrofuran-2-one (II) by heating at 155 C gives the triazolopyrimidinone (III) (1),which is treated with refluxing POCl3 to yield 7-chloro-6-(2-chloroethyl)5-methyl-1,2,4-triazolo[1,5-a]pyrimidine (IV).Finally this compound is cyclized with 1-phenylethylamine (V) by means of Na2CO3 in refluxing ethanol to afford the target pyrrolo-triazolo-pyrimidine derivative.
参考文献标题:Studies on cardiovascular agents.6.Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems
文献作者:Sato,Y.; Shimoji,Y.; Fujita,H.; Nishino,H.; Mizuno,H.; Kobayashi,S.; Kumakura,S.
参考来源:J Med Chem 1980,23(8),927