Friedel-Crafts alkylation with α-bromoarylacetates for the preparation of enantioenriched 2,2-diarylethanols
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Updated: Jan 26, 2026

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Published on: June 2, 2019
Yongtae Kim1, Yun Soo Choi, Su Kyung Hong
1Department of Chemistry, Konkuk University, Seoul 05029, Republic of Korea. parkyong@konkuk.ac.kr.
Abstract:
Highly enantioenriched 2,2-diarylethanols can be efficiently synthesized through the Friedel-Crafts alkylation of (hetero)arenes with configurationally labile α-bromoarylacetates. The substitution of highly diastereoenriched α-bromoarylacetates occurs in the presence of AgOTf, and the subsequent reduction affords diverse 2,2-diarylethanols with high yields and enantioselectivities up to 99 : 1 er. In addition, the application of this asymmetric synthetic methodology to the preparation of highly enantioenriched dihydrobenzofuran and indoline derivatives is demonstrated.
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