title: Facile Preparation of Peptides with C-Terminal N-Alkylamide via Radical-Initiated Dethiocarboxylation.
abstract: A new synthetic method has been developed to prepare peptides bearing a C-terminal N-alkylamide from peptide thioacids via a radical-initiated dethiocarboxylation process. This method enables the introduction of various alkyl groups to C-terminal amides simply by replacing the amino acid building block. Its application to the preparation of anti-cancer drug ABT-510 is also reported.
authors.affiliation: Institute of Biomedical Sciences and Graduate School of Pharmaceutical Sciences, Tokushima University.
authors.forename: Tatsuhiko
authors.initials: T
authors.lastname: Shimizu
authors.forename: Rin
authors.initials: R
authors.lastname: Miyajima
authors.forename: Naoto
authors.initials: N
authors.lastname: Naruse
authors.forename: Kosuke
authors.initials: K
authors.lastname: Yamaoka
authors.forename: Keisuke
authors.initials: K
authors.lastname: Aihara
authors.forename: Akira
authors.initials: A
authors.lastname: Shigenaga
authors.forename: Akira
authors.initials: A
authors.lastname: Otaka
mesh_terms: D000577:Amides / Q000737:chemistry*; D002264:Carboxylic Acids / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D010455:Peptides / Q000737:chemistry*
chemical_list: D000577:Amides; D002264:Carboxylic Acids; D010455:Peptides