新产品编号:869027

Chemical Name: 3-(3,5-Dichlorophenyl)-3-[5-oxo-1-[3-(1,4,5,6-tetrahydropyrimidin-2-ylamino)phenyl]pyrrolidin-3-ylcarboxamido]propionic acid
CAS No. 345296-69-7, 345296-70-0 (trifluoroacetate)
项目整合开发状态: Preclinical
项目研究机构: Amgen (Originator)
合成路线:Cyclization of itaconic acid (I) with 3-nitroaniline (II) at 100 C gives rise to 1-(3-nitrophenyl)-5-oxopyrrolidine-3-carboxylic acid (III).Subsequent condensation of acid (III) with methyl 3-amino-3-(3,5-dichlorophenyl)propanoate (IV) in the presence of EDC and HOAt yields amide (V).Reduction of the nitro group of (V) to the corresponding amine (VI) is effected by means of Zn and HOAc.Amine (VI) is then condensed with the cyclic thiourea (VII) employing HgCl2 to furnish the di-Boc-protected guanidine (VIII).Saponification of the methyl ester function of (VIII) then gives acid (IX).The N-Boc groups of (IX) are finally removed by treatment with trifluoroacetic acid to furnish the title compound.