降血压药坎地沙坦的合成

摘要

以3-硝基-2-乙氧甲酰氨基苯甲酸甲酯为原料，经Curtius重排、还原、环化、取代、水解反应，制得坎地沙坦(1)，总收率54.3％。该工艺原料价廉易得、合成路线短、产率提高、成本降低。%Candesartan(1) was synthesized from methyl 2-(azidocarbonyl)-3-nitrobenzoate via Curtius rearrangement, reduction, cyclization, substituent and hydrolysis reactions. The overall yield was 54.3%. The method has many advantages, such as cheap raw materials,short synthesis route, high yield and low cost.