AVE-0991

AVE 0991钠盐 Chemical Name: N-Ethyl-N'-[3-[4-(5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-ylmethyl)phenyl]-5-isobutylthien-2-ylsulfonyl]urea
CAS No. 304462-19-9, 306288-04-0 (monosodium salt)
项目整合开发状态: Biological Testing
项目研究机构: Aventis Pharma (Originator)
合成路线:4-Chloro-5-formyl-2-phenylimidazole (I) is alkylated with 4-bromobenzyl bromide (II) in the presence of K2CO3 in DMF to produce the N-bromobenzyl imidazole (III).Subsequent Suzuki coupling between aryl bromide (III) and 5-isobutyl-2-[(N-tert-butyl)sulfonamido]thiophene-3-boronic acid (IV) affords the thienylphenyl derivative (V).The N-tert-butyl group is then removed by treatment with trifluoroacetic acid in the presence of anisole,yielding sulfonamide (VI).Displacement of the chloro substituent of (VI) with MeOH/NaOH furnishes the 4-methoxy imidazole (VII).Finally,condensation of sulfonamide (VII) with ethyl isocyanate gives rise to the target N-sulfonyl urea compound.
📌 参考资料/链接:
参考文献标题:1-(p-Thienylbenzyl)-imidazoles as angiotensin-(1-7) receptor agonists,method for the production and the utilization thereof and pharmaceutical preparations containing said cpds.
文献作者:Wiemer,G.; Heitsch,H.(Aventis Pharma Deutschland GmbH)
参考来源:EP 1185527; JP 2002544130; US 6235766; US 6429222; WO 0068226

📄 详细内容


产品链接: CAS No. 304462-19-9››

产品链接: CAS No.306288-04-0››