2-THIAZOLIDINE DERIVATIVES HAVING BETA;-AMINO GROUP, PHARMACEUTICAL ACCEPTABLE SALTS AND PREPARATION PROCESS THEREOF

摘要

2-Thiazolidine derivatives having beta-amino group are provided to inhibit activity of DPP-IV(dipeptidyl peptidase-IV) associated with activity regulation of various hormones, so that the compounds are useful for treating diseases mediated by DPP-IV including type 2 diabetes mellitus. The 2-thiazolidine derivatives having beta-amino group represented by the formula(1) are prepared by reacting an amino acid represented by the formula(2) with 2-thiazolidine compounds represented by the formula(3) to prepare compounds represented by the formula(4), and deprotecting the compounds represented by the formula(4), wherein BOC is a protecting group; A is -NR^e(CH2)nR2 or -OR^b; R^a is hydrogen, C1-6 alkyl, C1-6 alkoxy, -OCF3, halogen, -CN or -CF3; R^b is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, isopropyl, t-butyl, -CH2CH2OH, -CH2CH2NH2, -CH2CH2N(CH2CH2)2O, -CH2CH2N(CH2CH3)2 or -CH2CH2NHCOCH3; R^c is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, benzyl, isopropyl or t-butyl; R^d and R^e are each independently hydrogen, C1-6 alkyl or C3-6 cycloalkyl; Y is carbon, oxygen, sulfur or nitrogen; Z is hydrogen, C1-6 alkyl, C3-6 cycloalkyl or -CO2R^b; and n is an integer of 0, 1 or 2.