Catalytic Synthesis of Chiral Phosphole Oxides via Desymmetric C–H Arylation of o-Bromoaryl Phosphine OxidesSupported by: National Natural Science Foundation of China Grant / Award numbers ‘51303043’, ‘21472031’, ‘21503060’
Supported by: Science and Technology Department of Zhejiang Province Grant / Award number ‘2015C31138’
Received: 08 February 2017
Accepted after revision: 05 March 2017
11 April 2017 (eFirst)
A palladium-catalyzed intramolecular direct arylation reaction of o-bromoaryl phosphine oxides was developed to afford a variety of P-stereogenic phosphole oxides in good yields. The enantioselectivities were closely associated with the specific structures of substrates, which ranged from 4–94%. As a result of ready availability of starting materials and simple operation to improve the enantioselectivities of the products with low ee values, the method provides a simple and straightforward procedure for the synthesis of P-stereogenic phosphole oxides.