Anatibant mesilate, LF-16-0687MS, LF-16-0687(free base)

(S)-N-(3-(4-氨酰胺基苯甲胺基苯甲胺)丙基)-1-((2,4-二氯-3-(((2,4-二甲基喹啉-8-基)氧)甲基)苯基)磺酰)吡咯氨酸-2-羧酰胺二盐酸盐 (2S)-N-(3-(4-甲脒基苯甲酰胺基)丙基)-1-(2,4-二氯-3-((2,4-二甲基-8-喹啉基氧基)甲基)苯磺酰基)吡咯烷-2-甲酰胺 Chemical Name: N-[3-(4-Amidinobenzamido)propyl]-1-[2,4-dichloro-3-(2,4-dimethylquinolin-8-yloxymethyl)phenylsulfonyl]-L-prolinamide bis(methanesulfonate)
CAS No. 209788-45-4 (diHCl), 209733-45-9 (free base)
项目整合开发状态: Phase I
项目研究机构: Fournier (Orphan Drug), Fournier (Originator)
合成路线:The title compound has been synthesized by condensation of amidino benzoic acid (I) with primary amine (II) using EDC and HOAt.

合成路线:In an alternative procedure,amine (II) was condensed with 4-cyanobenzoic acid (III) to give amide (IV).Subsequent addition of hydroxylamine to the cyano group of (IV) afforded N-hydroxy amidine (V),which was acetylated with Ac2O to produce (VI).This compound was finally reduced to the target amidine by hydrogenation over Lindlar catalyst.