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

• 영문명: 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
• 발행기관: 대한약학회
• 저자명: 서명은(Myung Eun Suh) 김혜경(Hae Gyung Kim) 김중협(Jung Hyup Kim)
• 간행물 정보: 『약학회지』제31권 제5호 (1987년), 338~342쪽, 전체 5쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1987.10.30

영문 초록

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.