抗高血压药缬沙坦的新合成方法  

New method for synthesis of antihypertensive drug valsartan

作　　者：邹江[1] 杨琰[1] 鲁峰[1] 王文峰[1] 

机构地区：[1]北京赛科药业有限责任公司,北京101111

出　　处：《化学试剂》2009年第4期303-304,共2页Chemical Reagents

摘　　要：以2N-三苯甲基-5-(4′-溴甲基联苯-2-基)四氮唑为原料,与L-缬氨酸甲酯盐酸盐反应制得N-[[2′-(2N-三苯甲基-四氮唑-5-基)-(1,1′-二苯基)-4-基]-甲基]-L-缬氨酸甲酯,然后经过脱三苯甲基保护、酰化、水解得到标题化合物,总收率49.8%。The reaction of 2N-trityl-5-（4′-methylbiphenyl-2-yl） tetrazole with L-valine methyl ester hydroehloride resulted in the formation of N- [ [ 2′- （2 N- trityl- tetrazol-5 - yl） [ 1,1′- biphenyl ] -4- yl] methyl]-L-valine methyl ester. Removal of the trityl protect- ing group produced N-[ [2′-（ 1H-tetrazol-5-yl）-（ 1, 1′-biphenyl）- 4-yl]-methyl]-L-valine methyl ester. Aeylation of N-[ [2′-（ 1H- tetrazol-5-yl ）-（ 1,1′-hiphenyl ）-4-yl ]-methyl ]-L-valine methyl ester with pentanoyl chloride resulted in the formation of N-（ 1- oxopentyl）- N- [ [ 2′-（ 1H-tetrazol-5-yl ）-（ 1, 1′-biphenyl ）-4-yl ] methyl ] - L- valine methyl ester. The reaction of N- （ 1- oxopentyl ） - N-[ [ 2′- （ 1 n-tetrazol-5-yl ）- （ 1, 1′-biphenyl ）-4-yl ] methyl ]- L- valine methyl ester with KOH led to the formation of valsartan, the total yield of which was 49.8 %.

关 键 词：缬沙坦 血管紧张素Ⅱ受体拮抗剂 合成 

分 类 号：O626.2[理学—有机化学]