新产品编号:2313393

Chemical Name: 2-[N-[4-(Carboxymethoxy)benzoyl]glycyl-L-valyl-L-prolyl-L-valyl]benzoxazole
项目整合开发状态: Preclinical
项目研究机构: Dainippon Pharmaceutical (Originator)
合成路线:N-Cbz-L-Valinal cyanohydrin (I) is converted into imidate (II) and then condensed with 2-aminophenol (III) to afford benzoxazole (IV).Removal of the N-Cbz group of (IV) with H2 and Pd/C provides amine (V),which is then coupled to N-Cbz-valyl proline (VI),yielding the dipeptide amide (VII).After hydrogenolysis of the N-Cbz protecting group of (VII),the free amine (VIII) is coupled to the acid fragment (IX) by means of EDC/pyridine to furnish (X).

合成路线:Oxidation of the secondary alcohol of (X) employing the Dess-Martin periodinane reagent leads to ketone (XI).The t-butyl ester group of (XI) is finally cleaved in the presence of trifluoroacetic acid to generate the title compound.