title: Synthesis of P-Chiral Dihydrobenzooxaphospholes Through Negishi Cross-Coupling.
abstract: An efficient Negishi cross-coupling was developed for the synthesis of the biaryl axes present in useful P-chiral dihydrobenzooxaphosphole ligands. This approach has allowed for the synthesis of new derivatives of these ligands that were not accessible by the previous route employing Suzuki-Miyaura cross-coupling. The use of Pd2(dba)3/BI-DIME as the catalyst system affords the desired biaryl compounds in good yields with excellent rates and with catalyst loadings as low as 0.25 mol %.
authors.affiliation: Chemical Development, Boehringer Ingelheim Pharmaceuticals, Incorporated , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.
authors.forename: Joshua D
authors.initials: JD
authors.lastname: Sieber
authors.affiliation: Chemical Development, Boehringer Ingelheim Pharmaceuticals, Incorporated , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.
authors.forename: Bo
authors.initials: B
authors.lastname: Qu
authors.affiliation: Chemical Development, Boehringer Ingelheim Pharmaceuticals, Incorporated , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.
authors.forename: Sonia
authors.initials: S
authors.lastname: Rodríguez
authors.affiliation: Chemical Development, Boehringer Ingelheim Pharmaceuticals, Incorporated , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.
authors.forename: Nizar
authors.initials: N
authors.lastname: Haddad
authors.affiliation: Chemical Development, Boehringer Ingelheim Pharmaceuticals, Incorporated , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.
authors.forename: Nelu
authors.initials: N
authors.lastname: Grinberg
authors.affiliation: Chemical Development, Boehringer Ingelheim Pharmaceuticals, Incorporated , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.
authors.forename: Heewon
authors.initials: H
authors.lastname: Lee
authors.affiliation: Chemical Development, Boehringer Ingelheim Pharmaceuticals, Incorporated , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.
authors.forename: Jinhua J
authors.initials: JJ
authors.lastname: Song
authors.affiliation: Chemical Development, Boehringer Ingelheim Pharmaceuticals, Incorporated , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.
authors.forename: Nathan K
authors.initials: NK
authors.lastname: Yee
authors.affiliation: Chemical Development, Boehringer Ingelheim Pharmaceuticals, Incorporated , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.
authors.forename: Chris H
authors.initials: CH
authors.lastname: Senanayake