Novel Synthesis of 8-tert-Butyl-6,7-Dihydro-5-Methyl-8H-Pyrrolo[3,2-e]-s-Triazolo-[1,5-a] Pyrimidine (Bumepidil), a New Cardiovascular Agent

관상혈관 확장제인 8-tert-Butyl-6, 7-Dihydro-5-Methyl-8H-Pyrrolo[3,2-e]-s-Triazolo-[1,5-a] Pyrimidine (Bumepidil)의 합성

8-tert-Butyl-6,7-dihydro-5-methyl-8H-pyrrolo [3,2-e]-s-triazolo [1,5-a] pyrimidine (Bumepidil), one of the s-triazolo [1,5-a] pyrimidine derivatives, has been recently found to be the most promising potential coronary vasodilator and antihypertensive agent. In this report, a new synthetic approach for Bumepidil, via direct N-amination of amino pyrimidine intermediate, was studied and found to be useful method. The novel synthetic method comprise the following steps, acylation of $\gamma$-butyrolactone, condensation with guanidine, direct N-amination, cyclization, chlorination, and finally cyclization using tert-butyl amine.