Design And Synthesis Of Apoptosis Of Tumor Promoter Of PAC-1 And Its Derivatives

Objective:To synthesize one to several agonists for Caspase-3 using PAC-1 for the lead compound.Methods:Firstly,The target compounds were synthesized from benzyl chloride and piperazine,Compound 3 was synthesized after 3 directional addition reaction;Secondly,Compound 5 was easily obtained on a large scale from salicylaldehyde,via a allylation and a Claisen rearrangement;Finally,PAC-1 was synthesized from a condensation reaction between Compound 3 and Compound 5. Using PAC-1 as the lead compound,two target molecules were synthesized. There are named TM1 and TM2.Para-hydroxybenzaldehyde and Vanillin separately instead of Salicylaldehyde,via a allylation,a Claisen rearrangement and a condensation reaction with Compound 3.Result:The structure of three target molecules were identified successfully by HPLC,UV,MS.Conclusion:The successful synthesis of PAC-1 for the subsequent synthesis of a series of derivatives including TM-1 and TM-2 has laid a good foundation.