POLYMER ORGANOCATALYST AND PREPARATION PROCESS

摘要

A chiral polymer organocatalyst comprising a main chain and side chain organocatalytic groups covalently attached to the main chain, which organocatalytic groups comprise an amino acid or amino acid derivative of the following general formula (I), in which one stereoisomeric form predominates: formula (I) wherein the catalyst is bound to the polymer main chain via R1, R2, R4, R5 or R6 through a linker (L) or direct bond, and wherein R1 -R6 and Z are defined as follows: R1 is H, a naturally occurring alpha-amino acid side chain or a non-natural commercially available alpha-amino acid side chain that may contain L; R2 is H, O (doubly bonded to give a carbonyl), O-L (where L is a linker), NH-L or L; R3 is H or doubly bonded to give a carbonyl with R2 when R2 is O; R4 is H, C1-C6 alkyl or L R5 is H, CO2H, C1-C6 alkyl, benzyl, L, CONHR (in which R is alkyl, aryl, hetereoaryl, arylalkyl or, heteroarylalkyl), tetrazolyl, CH2 coupled to a triazole moiety, an esterified CH2OH or CO2R (in which R is alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl), formula (II) or formula (III) wherein z is formula (IV) or a directed bond, X4 is H, Me3Si or Et3Si, X3 comprises a naturally-occurring alpha-amino acid side chain, H, C1-C6 alkyl or phenyl, Ar1 and Ar2 are each independently aryl or heteroaryl, and Y denotes the position of attachment to the main chain or linker; and R6 is H, CO2H3 C1-C6 alkyl, benzyl or L; and wherein the polymer organocatalyst comprises a cross-linked polymer.