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Org Lett. 2017 Apr 07;19(7):1542-1545. doi: 10.1021/acs.orglett.7b00351. Epub 2017 Mar 14.

Enantioselective Direct α-Arylation of Pyrazol-5-ones with 2-Indolylmethanols via Organo-Metal Cooperative Catalysis.

Organic letters

Zi-Qi Zhu, Yang Shen, Jin-Xi Liu, Ji-Yu Tao, Feng Shi

Affiliations

  1. School of Chemistry and Material Science, Jiangsu Normal University , Xuzhou 221116, China.

PMID: 28290202 DOI: 10.1021/acs.orglett.7b00351

Abstract

The first catalytic asymmetric α-arylation of pyrazol-5-ones has been established by using 2-indolylmethanols as direct electrophilic arylation reagents under the cooperative catalysis of Pd(0) and a chiral phosphoric acid, which afforded the α-arylation products of pyrazol-5-ones in generally high yields and good enantioselectivities (up to 99% yield, >99% ee).

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