含氟β-氨基酸和β-内酰胺的合成研究进展有机化学.pdfVIP

DOI: 10.6023/cjoc201303020 综述与进展 有机化学 Chinese Journal of Organic Chemistry REVIEW 含氟β-氨基酸和β- 内酰胺的合成研究进展 林岱宗 王 江 柳 红* ( 中国科学院上海药物研究所 新药研究国家重点实验室 上海 201203) 摘要 含氟β-氨基酸和含氟β- 内酰胺广泛应用于有机化学、药物发现和蛋白质生物学的研究中. 因而含氟β-氨基酸和 含氟 β- 内酰胺的合成工作深受广大研究者重视, 目前已开发出该类化合物的合成和拆分方法. 依据含氟 β-氨基酸种类 (α-氟取代β-氨基酸、α-三氟甲基取代β-氨基酸和β-三氟甲基-β-氨基酸), 重点介绍近年来该领域的代表性工作. 关键词 含氟β-氨基酸; 含氟β- 内酰胺; 合成 Recent Developments in the Synthesis of Fluorine-Containing β-Amino Acids and β-Lactams Lin, Daizong Wang, Jiang Liu, Hong* (State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203) Abstract Fluorine-containing β-amino acids and β-lactams have attracted appreciable attention due to their wide application in organic chemistry, drug discovery, and protein biology. Accordingly, the development of efficient synthetic methods is of considerable interest in academia and industry. The synthesis and resolution are achieved. This review briefly summarizes the recent development in the methodologies for the synthesis of fluorine-containing β-amino acids and β-lactams with classifica- tion by the species of the fluorine-containing β-amino acids (α-fluorinated β-amino acids, α-trifluoromethyl β-amino acids, and β-trifluoromethyl β-amino acids). Keywords fluorine-containing β-amino acid; fluorine-containing β-lactam; synthesis β-氨基酸在天然产物、有机合成研究和生物医药等 (Sitagliptin, 3), 于 2006 年获得美国 FDA 批准, 成为第 领域具有广泛应用. 氟原子以其独特的理化性质及其在