反应详情

5-Chloro-thiophene-2-carboxylic acid {2-[(1-isopropyl-piperidin-4-yl)-(2-morpholin-4-yl-2-oxo-ethyl)-sulfamoyl]-ethyl}-amide was prepared by an analogous procedure as described in example 15 starting from 83 mg (2 equiv.) 2-chloro-1-morpholin-4-yl-ethanone and 100 mg (0.25 mmol) 5-chloro-thiophene-2-carboxylic acid [2-(1-isopropyl-piperidin-4-ylsulfamoyl)-ethyl]-amide. Final purification by preparative RP-HPLC (CH3CN/H2O gradient+0.1% TFA) gave pure 5-chloro-thiophene-2-carboxylic acid {2-[(1-isopropyl-piperidin-4-yl)-(2-morpholin-4-yl-2-oxo-ethyl)-sulfamoyl]-ethyl}-amide. The title compound was obtained as its trifluoroacetate in form of a colorless amorphous material, which turned out to be hygroscopic with time.

1. custom5-Chloro-thiophene-2-carboxylic acid {2-[(1-isopropyl-piperidin-4-yl)-(2-morpholin-4-yl-2-oxo-ethyl)-sulfamoyl]-ethyl}-amide was prepared by an analogous procedure
2. customFinal purification by preparative RP-HPLC (CH3CN/H2O gradient+0.1% TFA)