制备手性联萘二甲酸的工艺改进

Process improvement on the preparation of chiral binaphthyl dicarboxylic acid

从手性联萘酚原料出发,通过3步反应合成标题化合物,总收率62%,产品光学纯度>99%。其中关键反应手性2,2'-二(三氟甲磺酸基)-1,1'-联萘与CO的直接羰基化反应,经过条件优化,可使用CO气袋完成,避免了昂贵的高压反应设备的使用。各步反应操作简便,条件温和,适合工业化生产。

A facile synthesis of chiral 1,1′-binaphthalene-2,2′-dicarboxylic acid has been described via a three-step reaction from optically active 1,1′-binaphthalene-2,2′-diol（overall yield up to 62%,ee up to 99%）.The key methoxycarbonylation of ditriflate of 1,1′-binaphthalene-2,2′-diol can be realized with air bag,avoiding the use of expensive high-pressure equipments.This optimal synthetic procedure is simple and suitable for industrial process.