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目的合成α-酮基酰胺肽类钙蛋白酶抑制剂的必需结构片段(2S,3S)-3-氨基-2-羟基-4-苯丁酰胺。方法以(S)-2-氨基-3-苯丙醇为起始原料,经过苄基保护、Parikh-Doering氧化、氰化水解、酰胺化和脱保护共5步反应合成目标化合物。结果与结论目标化合物和中间体的结构均经1H-NMR和13C-NMR谱确证,该合成路线方法简捷,适于大量制备。
AIM: To synthesize (2S, 3S) -3-amino-2-hydroxy-4-phenylbutanamide, an essential structural fragment of α-ketoamide peptide calpain inhibitor. Methods The target compounds were synthesized by the reaction of benzyl protection, Parikh-Doering oxidation, cyanidation, amidation and deprotection with (S) -2-amino-3-phenylpropanol as starting material. Results and Conclusions The structures of the target compounds and intermediates were confirmed by 1H-NMR and 13C-NMR spectra, respectively. The method was simple and suitable for mass preparation.