(R)-2-{[4-(3-甲氧基丙氧基)-3-甲基吡啶-2-基]甲基亚硫酰基}-1H-苯并咪唑的合成

Synthesis of(R)-2-{[4-(3-Methoxypropoxy)-3-methyl-pyridin-2-yl]-methylsulfinyl}-1H-benzimidazole

以2,3-二甲基吡啶为起始原料,经过11步反应,不对称合成了质子泵抑制剂的关键中间体:(R)-2-{[4-(3-甲氧基丙氧基)-3-甲基吡啶-2-基]甲基亚硫酰基}-1H-苯并咪唑.研究了用手性高效液相色谱拆分对映体、测定产品光学纯度的方法,结果表明目标产品的ee值达到99%.通过IR,UV,MS以及1H NMR分析对重要中间体和目标产品进行了结构鉴定.

A process for synthesis of （R）-2-{[4-（3-methoxypropoxy）-3-methyl-pyridin-2-yl]methyl- sulfinyl}-lH-benzimidazole from 2,3-1utidine was studied. The optical purity of the product was analyzed by chiral high performance liquid chromatography （HPLC） and the enantiomeric excess value reached 99%. The structures of reaction intermediates and target product were characterized by IR, UV, MS and 1H NMR spectra.