Litcius/Paper detail

Asymmetric Intramolecular Hydroalkoxylation of 2‐Vinylbenzyl Alcohols with Chiral Boro‐Phosphates

Caifang Han, Wei Meng, Xiangqing Feng, Haifeng Du

2022Angewandte Chemie International Edition17 citationsDOI

Abstract

Abstract Asymmetric intramolecular hydroalkoxylation of alkenes represents a very important approach to access optically active cyclic ethers. It was found that B(C 6 F 5 ) 3 could catalyze the cyclization of 2‐vinylbenzyl alcohols with only 0.05 mol % catalyst loading, affording the desired product in high yields. To accomplish the asymmetric reaction, a novel type of chiral boro‐phosphates was developed by treating chiral phosphoric acid with Piers’ borane, in which the oxygen atom of P=O and the boron atom act as Lewis base and acid centers, respectively. A highly enantioselective hydroalkoxylation was successfully realized to give optically active 1,3‐dihydroisobenzofuran derivatives in 78–99 % yields with 60–97 % ee's, in which an activation of O−H bond of alcohols by the boro‐phosphate species is hypothesized.

Topics & Concepts

Enantioselective synthesisIntramolecular forceChemistryPhosphoric acidCatalysisMedicinal chemistryBoronBoraneBOROOptically activeOrganic chemistryOrganoboron and organosilicon chemistryAsymmetric Synthesis and CatalysisAsymmetric Hydrogenation and Catalysis