Dual-hydroxymethyl Functional Groups Chelating Carboxypeptidase-a Inhibitors Design And Synthesis

Carboxypeptidase-A inhibitors using the double hydroxylmethyls as function groups were designed and synthesized firstly, began with diethyl malonate, introduced a alkyl and a hydroxymethyl at a-position respectivly, then single hydrolysis of ester group, selected reduction of acetic acid, etc. three target compounds were obtained: (1) 2,2-bis(hydroxymethyl)-3-phenyl- propanoic acid; (2) 5-benzyl-l,3-dioxane-5-carboxylic acid; (3) 2,2-bis(hydroxyl-methyl)-4-methylpent-4-enoic acid and two important reduction products:(4) ethyl 2,2-bis(hydroxylmethyl)-3-phenyl-propanoate; (5)ethyl 2,2-bis(hydroxymemyl)-4-methylpent-4-enoate.and carried on characteristics through IR,¹HNMR,¹³CNMR, MS and element analysis.1% cross-linked poly[4-hydroxy(tosyloxy)iodo]styrene be first prepared, Sulfides can be selectively oxidated to their corresponding sulfoxides with excellent yields under mild condtions by liner and 1 % cross-linked poly[4-hydroxy(tosyloxy) iodo]styrene, and the reagent of regeneration and cycling are also described。...