期刊
CHEMICAL COMMUNICATIONS
卷 48, 期 45, 页码 5578-5580出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2cc32225k
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资金
- NIH [GM 084333]
The first enantioselective synthesis of a potent GlyT1 inhibitor is described. A 3-nitroazetidine donor is used in an enantioselective aza-Henry reaction catalyzed by a bis(amidine)-triflic acid salt organocatalyst, delivering the key intermediate with 92% ee. This adduct is reductively denitrated and converted to the target through a short sequence, thereby allowing assignment of the absolute configuration of the more potent enantiomer.
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