A number of chiral phosphoramidite ligands containing electronically different N-heterocycles at the 3,3'-positions of the binol scaffold were synthesized. The nucleophilicity of the pendant heterocycles correlated with the propensity of the P(III) centre to undergo aerobic oxidation to P(V). Due to an unexpected Staudinger-type reaction between the product phosphoramidites, the order in which the individual synthetic transformations were conducted was found to be important. The synthesis of a phosphoramidite ligand containing flanking groups at the 3,3'-positions of the binol scaffold in addition to a stereogenic phosphorus atom was also undertaken. (C) 2011 Elsevier Ltd. All rights reserved.
A number of chiral phosphoramidite ligands containing electronically different N-heterocycles at the 3,3'-positions of the binol scaffold were synthesized. The nucleophilicity of the pendant heterocycles correlated with the propensity of the P(III) centre to undergo aerobic oxidation to P(V). Due to an unexpected Staudinger-type reaction between the product phosphoramidites, the order in which the individual synthetic transformations were conducted was found to be important. The synthesis of a phosphoramidite ligand containing flanking groups at the 3,3'-positions of the binol scaffold in addition to a stereogenic phosphorus atom was also undertaken. (C) 2011 Elsevier Ltd. All rights reserved.
[EN] NOVEL PROCESSES FOR MAKING SUBSTITUTED QUINAZOLINE COMPOUNDS USING HYDROGEN BONDING CATALYSTS<br/>[FR] NOUVEAUX PROCÉDÉS DE PRODUCTION DE COMPOSÉS DE QUINAZOLINE SUBSTITUÉS À L'AIDE DE CATALYSEURS DE LIAISON HYDROGÈNE
申请人:MERCK SHARP & DOHME
公开号:WO2017091453A1
公开(公告)日:2017-06-01
Disclosed herein is a novel process for preparing substituted quinazoline compounds of formula (I) using a hydrogen bonding catalyst.