SOLID PHASE SYNTHESIS OF 4-AMINOPROLINE DERIVATIVES AND/OR COMBINATORIAL LIBRARIES THEREOF

摘要

The present invention relates to solid phase synthesis of proline based compounds of Formula (1): R4R5NC(O)-Q-N(R1)-Y-R2 wherein R1 is an optionally substituted alkyl; R2 is alkyl, or optionally substituted aryl; R?4 and R5¿ are independently selected from cycloalkyl, or optionally substituted alkyl; R?4 and R5¿ taken together represent a five to seven membered saturated or unsaturated heterocyclic ring; Q represents (a) or (b), Y represents -S(O)¿n?-, -C(O)-, or -C(O)-NH-. Compounds of Formula (1) are prepared by a process which enables individual, parallel, and simultaneous synthesis of a plurality of compounds represented by Formula (1), starting from a compound of Formula (A): LG-C(O)-Z wherein LG represents a leaving group, Z represents (c), PG represents a protecting group.