3-Bromomethyl-5-(5-chloro-thiophen-2-yl)-isoxazole → 5-Chloro-thiophene-2-carboxylic acid {2-[[5-(5-chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-(1-isopropyl-piperidin-4-yl)-sulfamoyl]-ethyl}-amide

Participants

Reaction Steps

5-Chloro-thiophene-2-carboxylic acid {2-[[5-(5-chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-(1-isopropyl-piperidin-4-yl)-sulfamoyl]-ethyl}-amide was prepared by an analogous procedure as described in example 15 starting from 141 mg (2 equiv.) 3-bromomethyl-5-(5-chloro-thiophen-2-yl)-isoxazole 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-[[5-(5-chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-(1-isopropyl-piperidin-4-yl)-sulfamoyl]-ethyl}-amide. The title compound was obtained as its trifluoroacetate in form of a colorless amorphous material.

Provenance & Evidence