佛波酯磷脂酰－L－丝氨酸（PEPS）中间体的合成工艺改进

目的改进佛波酯磷脂酰-L-丝氨酸（PEPS）的中间体3-苄基-2-（8-叔丁基二苯基硅氧辛酰基）-1-三苯甲基-Sn-甘油（9）和N-叔丁氧羰基-L-丝氨酸二苯甲酯（11）的合成工艺。方法以D-甘露醇为原料，经丙叉基保护、氧化-还原、苄基保护、脱丙叉保护、选择性保护、酯化、羧基还原、硅烷基保护合成化合物9；以L-丝氨酸为原料，经氨基、羧基保护合成化合物11。结果与结论目标化合物的结构经。H-NMR谱确证，改进后的工艺，缩短了合成路线，简化了柱色谱分离、纯化步骤，具有原料易得，操作简便，成本低廉的优点。

Improved synthesis of two intermediates of phorbol ester-phosphatidyl-L-serine

Abstract :Aim To improve the synthetic procedure of 3-benzyl-2-(8-tert- butyldiphenylsilyloxyoctanoyl)-1-triphenylmethyl-sn-glycerol(9)and N-Boc-L -serinediphenylmethyl ester(11).Methods The compound（9） was synthesized from D-mannitol via eight steps reaction including isopropylidene acetal formation, oxidation-reduction, benzylation, deprotection, selective tritylation of the primary alcohol, esterification, reduction of the carboxylic acid, silylation. The compound（11）was synthesized from L-serine via Boc-protection of amino group and diphenylmethyl ester formation. Result and conclusion The structure of the target compounds were confirmed by 1H-NMR.A more convenient and efficient procedure was obtained by reducing synthetic steps and using easily available material.