Abstract: (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoic acid (AHPBA) is a key intermediate for preparing aminopeptidase N inhibitors，such as Bestatin，Phebestin and Probestin. Different synthetic routes，such as amino acid protocols ( D-phenylalanine，L-aspartic acid，malate diester)，organometallic methods (bifunctional aluminum complex)，acetophenone methods，enzyme routes (lipase and whole-cell enzyme)，and other approaches for preparing AHPBA are reviewed and analyzed. By comparison，organometallic catalysis，enzyme routes and acetophenone methods are superior in low-cost，mild condition，simple procedure with potential application for commercialization. The future development of this specific area will be focused on optimization and improvement of the reported routes.

Key words: (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoic acid(AHPBA), aminopeptidase, inhibitor, synthetic method

摘要： (2S,3R)-2羟基-3-氨基-4-苯基丁酸（AHPBA）是制备Bestatin、Phebestin和Probestin等氨肽酶N(Aminopeptide N)抑制剂的关键中间体。本文从氨基酸法（D-苯丙氨酸、L-天门冬氨酸、苹果酸二酯）、有机金属催化法（双功能铝配合物）、酶催化法（脂肪酶和全细胞酶）以及其它方法对此中间体的合成方法及路线进行综述和分析。经比较，有机催化法、酶法以及苯乙酮法因其具有经济有利、条件温和或路线简单特点，具有潜在的工业化应用前景。同时，未来人们对AHPBA的合成开发将集中在对已有工艺路线的改进与优化。

关键词: (2S, 3R)-2-羟基-3-氨基-4-苯基丁酸, 氨肽酶, 抑制剂, 合成方法