title: Negishi Approach to 1,5-Disubstituted 3-Amino-1H-1,2,4-triazoles.
abstract: An efficient synthesis of 1,5-disubstituted 3-amino-1H-1,2,4-triazoles has been achieved via a Negishi coupling of aryl or vinyl bromides and 1-substituted 3-amino-1H-1,2,4-triazoles in the presence of Knochel's base tetramethylpiperidinylzinc chloride lithium chloride (TMPZnCl·LiCl) and catalytic bis(di-tert-butylphenylphosphine)palladium chloride. This chemistry tolerates a variety of electronically diverse aryl or vinyl bromides and 1-substituted 3-amino-1H-1,2,4-triazoles.
authors.affiliation: Small Molecule Process Chemistry and ‡Small Molecule Analytical Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
authors.forename: Jeff
authors.initials: J
authors.lastname: Shen
authors.affiliation: Small Molecule Process Chemistry and ‡Small Molecule Analytical Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
authors.forename: Brian
authors.initials: B
authors.lastname: Wong
authors.affiliation: Small Molecule Process Chemistry and ‡Small Molecule Analytical Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
authors.forename: Chunang
authors.initials: C
authors.lastname: Gu
authors.affiliation: Small Molecule Process Chemistry and ‡Small Molecule Analytical Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
authors.forename: Haiming
authors.initials: H
authors.lastname: Zhang