Abstract

The asymmetric 1,6-conjugate addition of arylboronic acids to natural securinine under rhodium(I) catalysis displays a very high regioselectivity, along with a remarkable diastereoselectivity (>99:1) and high yields. The in vitro cytotoxicity of the resulting securinine analogues was assayed against HCT-116 colon cancer cells, giving a new insight into the structure–activity relationship of securinine.

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