NKT-343, SDZ-NKT-343

1-[[(2-硝基苯基)氨基]羰基]-l-丙基-N-甲基-3-(2-萘yl)-N-(苯基甲基)-l-丙氨酰胺Chemical Name: N-(2-Nitrophenyl)carbamoyl-L-prolyl-L-[3-(2-naphthyl)]alanine N-benzyl-N-methylamide
CAS No. 180046-99-5
项目整合开发状态: Phase I
项目研究机构: Novartis (Originator)
合成路线:The reaction of N-(tert-butoxycarbonyl)-L-(2-naphthyl)alanine (I) with N-methylbenzyamine (II) by means of isobutyl chloroformate and NMM in dichloromethane gives the corresponding amide (III),which is deprotected with HCl in dioxane yielding (IV) with a free amino group.Finally,this compound is condensed with 1-[N-(2-nitrophenyl)carbamoyl]-L-proline (V) by means of HOBT and DCC in THF.The intermediate 1-[N-(2-nitrophenyl)carbamoyl]-L-proline (V) has been obtained by reaction of L-proline (VI) with 2-nitrophenyl isocyanate (VII) by means of NMM in THF/water.