The first catalytic asymmetric (4+3) cyclization of in situ generated ortho-quinone methides with 2-indolylmethanols has been established, which constructed seven-membered heterocycles in high yields (up to 95 %) and excellent enantioselectivity (up to 98 %). This approach not only represents the first catalytic asymmetric (4+3) cyclization of o-hydroxybenzyl alcohols, but also enabled an unprecedented catalytic asymmetric (4+3) cyclization of 2-indolylmethanols. In addition, a scarcely reported catalytic asymmetric (4+3) cyclization of para-quinone methide derivatives was accomplished.
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| http://dx.doi.org/10.1002/anie.201901955 | DOI Listing |
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