Hydrochloric Acid → HCID 11949831, compound

Participants

Reaction Steps

Pyridine (0.3 mL, 3.72 mmol) was added to a suspension of the hydrochloride of 1-(4-aminobenzyl)-3-(4-tert-butylbenzyl)-1,3-dihydrobenzimidazol-2-one (Q) (717 mg, 1.7 mmol) in abs. THF (20 mL). The reaction mixture was stirred at RT for 10 min, methanesulphonyl chloride (0.13 mL, 1.7 mmol, dissolved in abs. THF (1 mL)) was added within a period of 5 min, and the reaction mixture was again stirred at RT over a period of 17 h. To the reaction mixture there was then added H2O (10 mL) followed, after 10 min, by H2O (100 mL). After an hour the precipitated solid matter was separated through a frit and then dried in vacuo. The desired product N-{4-[3-(4-tert-Butyl-benzyl)-2-oxo-2,3-dihydrobenzoimidazol-1-ylmethyl]phenyl}methanesulfonamide (60) was obtained in a yield of 680 mg (86% of theory, mp: 228-230° C.).

Provenance & Evidence