Pyrazole → HCID 178462125, compound

Participants

Reaction Steps

Trans-4-(6-Chloro-pyridine-3-sulfonylamino)-cyclohexanecarboxylic acid [(R)-1-(4-fluoro-phenyl)-ethyl]-amide (Example 114, 100 mg, 0.225 mmol), pyrazole (70 mg, 0.91 mmol), Pd2(dba)3 (25 mg, 0.025 mmol), Xantphos (20 mg, 0.05 mmol), sodium tert-butoxide (108 mg, 1.125 mmol) were dissolved in toluene (1 ml) and tert-butanol (3 ml). The reaction mixture was microwaved at 160° C. for 5 min., after which LCMS indicated that the reaction was complete. The reaction was diluted with DCM and MeCN and filtered through a syringe, the concentrated in vacuo to a yellow oil. The crude material was purified via reverse phase chromatography and lyophilized to yield the title compound as a white solid (15 mg, 14%). [M+H]=472.08

Provenance & Evidence