化工进展
化工進展
화공진전
CHEMICAL INDUSTRY AND ENGINEERING PROGRESS
2013年
5期
1127-1132
,共6页
(2S，3R)-2-羟基-3-氨基-4-苯基丁酸%氨肽酶%抑制剂%合成方法
(2S，3R)-2-羥基-3-氨基-4-苯基丁痠%氨肽酶%抑製劑%閤成方法
(2S，3R)-2-간기-3-안기-4-분기정산%안태매%억제제%합성방법
(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoic acid(AHPBA)%aminopeptidase%inhibitor%synthetic method
(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.
(2S,3R)-2羥基-3-氨基-4-苯基丁痠(AHPBA)是製備 Bestatin、Phebestin 和 Probestin 等氨肽酶N(Aminopeptide N)抑製劑的關鍵中間體.本文從氨基痠法(D-苯丙氨痠、L-天門鼕氨痠、蘋果痠二酯)、有機金屬催化法(雙功能鋁配閤物)、酶催化法(脂肪酶和全細胞酶)以及其它方法對此中間體的閤成方法及路線進行綜述和分析.經比較,有機催化法、酶法以及苯乙酮法因其具有經濟有利、條件溫和或路線簡單特點,具有潛在的工業化應用前景.同時,未來人們對AHPBA的閤成開髮將集中在對已有工藝路線的改進與優化.
(2S,3R)-2간기-3-안기-4-분기정산(AHPBA)시제비 Bestatin、Phebestin 화 Probestin 등안태매N(Aminopeptide N)억제제적관건중간체.본문종안기산법(D-분병안산、L-천문동안산、평과산이지)、유궤금속최화법(쌍공능려배합물)、매최화법(지방매화전세포매)이급기타방법대차중간체적합성방법급로선진행종술화분석.경비교,유궤최화법、매법이급분을동법인기구유경제유리、조건온화혹로선간단특점,구유잠재적공업화응용전경.동시,미래인문대AHPBA적합성개발장집중재대이유공예로선적개진여우화.
@@@@Absstract:(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.
