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KMID : 0370219870310050338
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Yakhak Hoeji
1987 Volume.31 No. 5 p.338 ~ p.342
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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
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서명은/Suh ME
김혜경/김중협/Kim HG/Kim JH
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Abstract
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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.
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KEYWORD
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