沙库必曲中间体的合成

Synthesis of Sacubitril Intermediates

以D-苯丙氨酸为原料,经碘代、酯化、BOC保护、偶联、还原合成了沙库必曲的重要中间体——(R)-叔丁基(1-[(1,1′-联苯)-4-基]-3-羟基丙烷-2-基)氨基甲酸酯。反应总收率为46.17%。此工艺具有原料易得、收率较高、质量较好等优点。

An important intermediate of sacubitril-- （R）-tert-butyl-（1-（[1,1 ＇-biphenyl]-4-yl）- 3-hydroxypropan-2-yl）carbamate synthesized by iodine generation, esterification, Boc protection, coupling and reduction from D-Phenylalanine. The overall yield of the reaction was 46.17 %. This method has several advantages of cheap reagents, high yield and good quality.