LY-164846-药物合成数据库

【药物名称】LY-164846

化学结构式(Chemical Structure):

参考文献No.	430
标题:	Benzothienylglycyl cephalosporin derivs.
作者:	Blaszczak, L.C.; Kukolja, S.; Turner, J.R. (Eli Lilly and Company)
来源:	ES 8600308; GB 2137995; US 4492693

合成路线图解说明: The condensation of N-(tert-butoxycarbonyl)-2-benzothien-3-ylglycine (I) with 4-nitrobenzyl-7-amino-3-methyl-3-cephem-4-carboxylate (II) in THF gives 4-nitrobenzyl-7-[N-(tert-butoxycarbonyl)-2-benzo[b]thien-3-ylglycylamido]-3 methyl-3-cephem-4-carboxylate (III), which is deprotected partially by treatment with p-toluenesulfonic acid in acetonitrife yielding 4-nitrobenzyl-7-(benzo[b]thien-3-ylglycyl-amido)-3-methyl-3-cephem-4-carboxytate (IV). Finally, this product is submitted to hydrogenolysis with H2 over Pd/C in methanol HCl.

参考文献No.	68119
标题:	LY-164846
作者:	Casta馿r, J.; Prous, J.
来源:	Drugs Fut 1986,11(7),570

合成路线图解说明: The condensation of N-(tert-butoxycarbonyl)-2-benzothien-3-ylglycine (I) with 4-nitrobenzyl-7-amino-3-methyl-3-cephem-4-carboxylate (II) in THF gives 4-nitrobenzyl-7-[N-(tert-butoxycarbonyl)-2-benzo[b]thien-3-ylglycylamido]-3 methyl-3-cephem-4-carboxylate (III), which is deprotected partially by treatment with p-toluenesulfonic acid in acetonitrife yielding 4-nitrobenzyl-7-(benzo[b]thien-3-ylglycyl-amido)-3-methyl-3-cephem-4-carboxytate (IV). Finally, this product is submitted to hydrogenolysis with H2 over Pd/C in methanol HCl.