A convenient synthesis of activated enantiomerically pure 2-ethynylaziridines |
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| Institution: | 1. Institute of Drug Synthesis and Pharmaceutical Process, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China;2. Faculty of Chemical Engineering and Light Industry, Guangdong University of Technology, Guangzhou 510090, China;1. Medicinal Chemistry Division, GVK Biosciences Private Limited, Plot No. 28 A, Industrial Development Area Nacharam, Hyderabad 500076, India;2. Department of Chemistry, Institute of Science and Technology, Jawaharlal Nehru Technological University, Kukatpally, Hyderabad 500085, India;3. Department of Medical Applied Chemistry, Chung Shan Medical University, Taichung 40201, Taiwan;4. Department of Medical Education, Chung Shan Medical University Hospital, Taichung 40201, Taiwan;5. Department of Medical Laboratory Science and Biotechnology, China Medical University, No. 91, Hsueh-Shih Road, Taichung 40402, Taiwan;6. School of Pharmacy, China Medical University, No. 91, Hsueh-Shih Road, Taichung 40402, Taiwan;7. Research Center for Chinese Herbal Medicine, China Medical University, Taichung 40402, Taiwan |
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| Abstract: | 2,3-cis- and 2,3-trans-N-Arylsulfonyl-2-ethynylaziridines with high enantiomeric purity have been synthesized. N-Protected amino aldehydes synthesized from natural α-amino acids were successively treated with Ph3PC(Br)CO2Me, DIBAL, MsCl–Et3N, NaH in DMSO, and tert-BuOK in THF to yield 2-ethynylaziridines in good to high yields. |
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