3-aryl-2-hydroxypropyl Design And Synthesis Of Piperazine Derivatives

In this paper, many types of antiaginal drugs and their action mechanisms were introduced, the antiginal effect of partial fatty acid oxidation(pFOX) inhibitor ranolazine was briefly introduced.The structure-activity-relationship of ranolazine derivatives and trapidil derivatives was discussed. With ranolazine and trapidil as the lead compounds, new 3-aryloxy-2-hydroxy propyl piperazine derivatives were designed and synthesized. Based on pricinciple of hybridization, 5-methyl/trifluoromethyl-1,2,4-triazolo-[1,5-α]-pyrimidin-7-yl was introduced at the 4 position of piperazine ring; 3-aryloxy-2-hydroxy propyl was also introduced at 1 position of the piperazine ring .To study its effect of activity, Several substitutuents were introduced at the benzene ring.Twenty new compounds which had not been reported in literature were designed and synthesized. Their chemical structures were comfirmed by MS. The pharmacological evaluation of these target compounds is in progress.We take the 3-amino-1, 2, 4-triazole as the starting material, the target compounds were obtained after cyclization, chlorization aminolysis and alkylation. The total yield was 12.4%～23.6%.