合成化学
閤成化學
합성화학
CHINESE JOURNAL OF SYNTHETIC CHEMISTRY
2010年
1期
83-85,133
,共4页
闫起强%郭拥政%谢苏豪%祁伟%杨琰%王文峰
閆起彊%郭擁政%謝囌豪%祁偉%楊琰%王文峰
염기강%곽옹정%사소호%기위%양염%왕문봉
氯沙坦%烷基化%脱保护%药物合成
氯沙坦%烷基化%脫保護%藥物閤成
록사탄%완기화%탈보호%약물합성
Losartan%N-alkylation%deprotection%drug synthesis
以2-丁基-4-氯-5-羟甲基咪唑和5-(4-溴甲基联苯-2-基)-1-三苯甲基-1H-四唑为原料,通过氮烷基化、脱三苯甲烷保护基和还原反应合成了抗高血压药氯沙坦,总收率64%,其结构经~1H NMR表征.
以2-丁基-4-氯-5-羥甲基咪唑和5-(4-溴甲基聯苯-2-基)-1-三苯甲基-1H-四唑為原料,通過氮烷基化、脫三苯甲烷保護基和還原反應閤成瞭抗高血壓藥氯沙坦,總收率64%,其結構經~1H NMR錶徵.
이2-정기-4-록-5-간갑기미서화5-(4-추갑기련분-2-기)-1-삼분갑기-1H-사서위원료,통과담완기화、탈삼분갑완보호기화환원반응합성료항고혈압약록사탄,총수솔64%,기결구경~1H NMR표정.
Losartan in overall yield of 64% was synthesized from 2-butyl-4-chloro-5-hydroxymethyl-imidazole and 5-(4-bromomethyl-biphenyl -2-yl)-1-triphenylmethyl-1H-tetrazole by a three-step reaction of N-alkylation,deprotection(triphenylmethane protecting group) and reduction.The structure was characterized by ~1H NMR.
