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Enzymatic resolution of bicyclic 1-heteroarylamines using Candida antarctica lipase B. | LitMetric

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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http://dx.doi.org/10.1021/jo026701rDOI Listing

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