氘代Rigosertib类似物的合成

Synthesis of Deuterated Rigosertib Analogs

以2,4,6-三羟基苯甲醛为原料制得中间体2,4,6-三甲氧基苯甲醛（2a）和2,4,6-三三氘甲氧基苯甲醛（2b）;以4-烷氧基-3-硝基苄硫基乙酸为原料,经氧化、缩合-脱羧、还原、取代和水解5步反应合成了氘代Rigosertib类似物,收率80%-86%,其结构经1H NMR和MS表征。

Two intermediates,2,4,6-trimethoxybenzaldehyde（ 2a） and 2,4,6-trideuteromethoxybenzaldehyde（ 2b）,were prepared from 2,4,6-trihydroxybenzaldehyde. Three deuterated Rigosertib analogs,in yield of 80% - 86%,were synthesized by the reaction of oxidization,condensation-decarboxylation,reduction,substitution and hydrolysis from [（ 4-alkaxy-3-nitrobenyl）-thion]acetic acid. The structures were confirmed by1 ^H NMR and MS.