期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 17, 期 30, 页码 7182-7191出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9ob01350d
关键词
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资金
- National Natural Science Foundation of China (NSFC) [21272024]
An enantioselective Mannich reaction between 3-fluorooxindoles and pyrazolinone ketimines has been developed for the construction of amino-pyrazolone-oxindoles containing stereogenic C-F units. Based on this new protocol that allows for the generation of two adjacent tetrasubstituted stereocenters, a variety of structurally diverse fluorinated amino-pyrazolone-oxindoles were obtained in good to excellent yields with excellent diastereoselectivities and enantioselectivities (up to 98% yield, >20 : 1 dr and >99% ee). What's more, good yield and high stereoselectivities were obtained in the gram-scale reaction.
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