FR-226807
Chemical Name: N-(3,4-Dimethoxybenzyl)-2-[2-hydroxy-1(R)-methylethylamino]-5-nitrobenzamide
CAS No. 247568-68-9, 247567-47-1 ((S)-isomer)
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合成路线:2-Fluoro-5-nitrobenzoic acid (I) was converted to the corresponding acid chloride (II) by chlorination of with SOCl2.Condensation of acid chloride (II) with 3,4-dimethoxybenzylamine (III) provided amide (IV).The aromatic fluorine atom of (IV) was then displaced with (R)-2-amino-1-propanol (V) in hot pyridine to furnish the title anthranilic acid derivative.
📌 参考资料/链接:
参考文献标题:Anthranilic acid derivs.as inhibitors of the cGMP-phosphodiesterase
文献作者:Oku,T.; Sawada,K.; Kuroda,A.; Kayakiri,N.; Sawada,Y.; Inoue,T.; Mizutani,T.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 1080069; JP 2001508811; US 6384080; WO 9954284