title: The development and preparation of the 2,4-dimethoxybenzyl arylhydrazine (DMBAH) "latent" safety-catch linker: solid phase synthesis of ketopiperazines.
abstract: The development and preparation of the 2,4-dimethoxybenzyl arylhydrazine (DMBAH) linker 3, a new class of "latent" safety-catch linker which is stable under Mitsunobu alkylation conditions and in the presence of amines and hydrazine, is reported. The utility of the new linker is exemplified by the synthesis of ketopiperazines (MKPs) 24 bearing up to four points of diversity using a cyclitive cleavage approach.
authors.affiliation: GSK Cambridge Technology Centre, University Chemical Laboratory, Lensfield Road, Cambridge, UK CB2 1EW.
authors.forename: Frédéric
authors.initials: F
authors.lastname: Berst
authors.forename: Andrew B
authors.initials: AB
authors.lastname: Holmes
authors.forename: Mark
authors.initials: M
authors.lastname: Ladlow
mesh_terms: D020650:Combinatorial Chemistry Techniques / Q000379:methods; D003432:Cross-Linking Reagents / Q000138:chemical synthesis / Q000737:chemistry*; D006834:Hydrazines / Q000138:chemical synthesis / Q000737:chemistry*; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry; D012117:Resins, Synthetic / Q000737:chemistry
chemical_list: D003432:Cross-Linking Reagents; D006834:Hydrazines; D010879:Piperazines; D012117:Resins, Synthetic