Enzymatic resolution of bicyclic 1-heteroarylamines using Candida antarctica lipase B |
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Authors: | Skupinska Krystyna A McEachern Ernest J Baird Ian R Skerlj Renato T Bridger Gary J |
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Institution: | AnorMED Inc., #200-20353 64th Avenue, Langley, BC, Canada V2Y 1N5. |
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Abstract: | Candida antarctica lipase B has been used to kinetically resolve a structurally diverse series of bicyclic 1-heteroaryl primary amines by enantioselective acetylation. High yields of either enantiomer could be obtained with excellent enantioselectivity (90-99% ee), while the undesired enantiomer could, in some cases, be recycled by thermal racemization. The absolute stereochemistry of the products was confirmed by an X-ray crystal structure. |
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