KRH-1636

Chemical Name: N1-[1(S)-(1-Naphthyl)ethyl]-N2-[4-(pyridin-2-ylmethylaminomethyl)benzoyl]-L-argininamide
CAS No. 369653-89-4 (mono HCl salt)
项目整合开发状态: Preclinical
项目研究机构: Kureha (Originator)
合成路线:2-Picolylamine (I) is protected with Boc2O,and the resultant tert-butyl carbamate (II) is further alkylated with methyl 4-(bromomethyl)benzoate (III) to furnish (IV).Subsequent saponification of the methyl ester group of (IV) affords the carboxylic acid (V).

合成路线:The protected arginine (VI) is coupled to (S)-1-naphthylethylamine (VII) in the presence of EDC/HOBt to give amide (VIII).Subsequent N-Fmoc group removal employing diethylamine in DMF leads to amine (IX),which is further condensed with carboxylic acid (V) yielding amide (X).Finally,trifluoroacetic acid-promoted cleavage of the N-Boc and N-Pbf protecting groups of (X) provides the title compound.