There is provided a process for manufacture of optically-active, 2-(acyloxymethyl)-1,3-oxathiolanes of Formula I comprising a preparation of a racemic compound and an enzyme-catalyzed kinetic resolution of the enantiomers. The invention may further provide for the esterification and racemization of the by-product of the enzymatic reaction. In this manner, 2(R)-(benzoyloxymethyl)-1,3-oxathiolane is prepared as a useful intermediate for manufacture of the anti-HIV drug Apricitabine.
提供了一种制备光学活性的2-(酰氧甲基)-1,3-噁
硫烷酮(式I)的方法,包括制备外消旋化合物和酶催化对映体的动力学分辨。本发明还可以进一步提供酯化和酶催化反应的副产物的外消旋化。通过这种方式,制备出2(R)-(苯甲酰氧甲基)-1,3-噁
硫烷酮作为制造抗HIV药物Apricitabine的有用中间体。