A Synthetic Route to Chiral Dihydrobenzothiazines through Ring Opening of Activated Aziridines with 2‐Halothiophenols/Copper‐Powder‐Mediated C−N Cyclization |
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| Authors: | Prof?Dr Manas K Ghorai Masthanvali Sayyad Yerramsetti Nanaji Sourita Jana |
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| Institution: | 1. (+91)?512‐2597436;2. Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur, India |
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| Abstract: | A simple protocol for the synthesis of dihydrobenzothiazines through regio‐ and stereoselective SN2‐type ring opening of N‐tosylaziridines with sulfur nucleophiles followed by copper‐powder‐mediated intramolecular C?N cyclization in excellent yields (up to 95 %) with high diastereo‐ and enantioselectivity (up to >99 %) is reported. |
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| Keywords: | copper asymmetric synthesis aziridines regioselectivity stereoselectivity |
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