Chemo-enzymatic synthesis of chiral 2-substituted succinic acid derivatives |
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| Affiliation: | 1. College of Biotechnology and Pharmaceutical Engineering, Nanjing Tech University, Nanjing 211816, China;2. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;3. Jiangsu Kanion Pharmaceutical Co., Ltd., Lianyungang 222002, China;1. Centre for Synthesis and Chemical Biology (CSCB), Department of Pharmaceutical and Medicinal Chemistry, The Royal College of Surgeons in Ireland, 123 St. Stephen’s Green, Dublin 2, Dublin, Ireland;2. Linnea SA, Via Cantonale 70, CH-6595 Riazzino (TI), Switzerland;1. Dipartimento di Scienze Molecolari e Nanosistemi, Università Ca’ Foscari Venezia, via Torino 155, 30170 Venezia Mestre, Italy;2. Dipartimento di Scienze Ambientali, Informatica e Statistica, Università Ca’ Foscari Venezia, via Torino 155, 30170 Venezia Mestre, Italy |
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| Abstract: | Prochiral discrimination by the biocatalyst Alcalase®, an enzyme preparation of subtilisin Carlsberg, was used to effect enantio- and regioselective monohydrolysis of a variety of (RS)-2-substituted succinate diesters to afford the corresponding half esters in modest to excellent enantiomeric excesses (>99%). Exploitation of malonate chemistry, as well as recycling of the unhydrolyzed isomer from the enantioselective hydrolysis, has resulted in a process which is both practical and economical. |
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