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新产品编号:1954279

Chemical Name: 3-[3-(2-Amino-6-methylpyrimidin-4-ylsulfanyl)-1(E)-propenyl]-7-[2-(2-aminothiazol-4-yl)-2(Z)-(methoxyimino)acetamido]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid; 3-[3-(2-Amino-6-methylpyrimidin-4-ylsulfanyl)-1(E)-propenyl]-7-[2-(2-aminoth
项目整合开发状态: Biological Testing
项目研究机构: LG Chem (Originator)
合成路线:Coupling of carboxylic acid (II) to the 7-aminocephem derivative (I) using POCl3 and pyridine produced the corresponding amide (III).Displacement of the chloro group of (III) with triphenyl phosphine furnished the phosphonium salt (IV),which was subjected to a Wittig reaction with chloroacetaldehyde (V),yielding the Z-propenyl chloride (VI).Subsequent reaction of allyl chloride (VI) with 4-amino-2-mercapto-6-methylpyrimidine (VII) in the presence of NaI produced the E-propenyl sulfide (VIII).The N-trityl group and the p-methoxybenzyl ester of (VIII) were finally cleaved by treatment with trifluoroacetic acid in anisole to furnish the title compound.
📌 参考资料/链接:
参考文献标题:Synthesis and antibacterial activities of novel C(3)-aminopyrimidinyl substituted cephalosporins
文献作者:Lee,C.-S.; Oh,S.H.; Ryu,E.J.; Kim,M.Y.; Paek,K.S.
参考来源:J Antibiot 2000,53(11),1305