title: Pd(II)-catalyzed enantioselective synthesis of P-stereogenic phosphinamides via desymmetric C-H arylation.
abstract: We present the enantioselective synthesis of P-stereogenic phosphinamides through Pd-catalyzed desymmetric ortho C-H arylation of diarylphosphinamides with boronic esters. The method represents the first example of the synthesis of P-stereogenic phosphorus compounds via the desymmetric C-H functionalization strategy. The reaction proceeded efficiently with a wide array of reaction partners to afford the P-stereogenic phosphinamides in up to 74% yield and 98% ee. The efficiency was further demonstrated by gram scale syntheses. Moreover, the flexible conversion of the P-stereogenic phosphinamides into various types of P-stereogenic phosphorus derivatives was also elaborated. Thus, the protocol provides a novel tool for the efficient and versatile synthesis of P-stereogenic compounds.
authors.affiliation: Changchun Institute of Applied Chemistry, Chinese Academy of Sciences , Changchun, Jilin 130022, China.
authors.forename: Zhi-Jun
authors.initials: ZJ
authors.lastname: Du
authors.forename: Jing
authors.initials: J
authors.lastname: Guan
authors.forename: Guo-Jie
authors.initials: GJ
authors.lastname: Wu
authors.forename: Peng
authors.initials: P
authors.lastname: Xu
authors.forename: Lian-Xun
authors.initials: LX
authors.lastname: Gao
authors.forename: Fu-She
authors.initials: FS
authors.lastname: Han