HCID 69288006, compound → HCID 23085247, compound

Participants

Reaction Steps

To a solution of [5-(5-chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-3,5-dimethyl-4-([1,4]oxazepane-4-sulfonyl)-1H-pyrrole-2-carboxylic acid ethyl ester (100 mg) in 20 mL of THF/water(3:1) was added LiOH monohydrate (200 mg) The mixture was stirred for 2h at 45° C. and for 6 h at 60° C. whereupon it was cooled to RT, concentrated, acidified with 2M HCl to pH=2 and extracted with DCM (3×30 mL). The combined organic layers were dried (MgSO4) and concentrated to give crude 1-[5-(5-chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-3,5-dimethyl-4-([1,4]oxazepane-4-sulfonyl)-1H-pyrrole-2-carboxylic acid (80 mg) which was used directly in the next step.

Provenance & Evidence