Epithalon, Epitalon

埃皮塔隆Chemical Name: L-Alanyl-L-glutamyl-L-aspartyl-glycine
CAS No. 307297-39-8
项目整合开发状态: Phase II
项目研究机构: Russian Academy of Medical Sciences (Originator)
合成路线:The title compound was obtained by solution-phase peptide synthesis.Acylation of L-aspartic acid beta-benzyl ester (II) with the succinimidyl ester of N-Boc-gamma-benzyl-L-glutamic acid (I) led to the protected dipeptide (III).Removal of the Boc protecting group of (III) by means of trifluoroacetic acid afforded amine (IV),which was subsequently condensed with N-Cbz-L-alanine succinimidyl ester (V) to furnish tripeptide (VI).Coupling of (VI) with glycine benzyl ester (VII) using DCC and HOBt gave the fully protected peptide (VIII).The N-Cbz and benzyl ester groups of (VIII) were finally removed by catalytic hydrogenation over Pd/C to provide the target tetrapeptide.