反应详情

Heated 2-((E)-(3,3-dimethylbutylimino)methyl)-6-fluoro-N-(2-morpholinoethyl)benzenamine (606 mg, 1.806 mmol) and (S)-2-mercaptosuccinic acid (282 mg, 1.878 mmol) in toluene (10 mL) at 80° C. for 1 day. Volatiles were removed on a rotary evaporator under high vacuum to give 2-(2-(2-(2-morpholinoethylamino)-3-fluorophenyl)-3-(3,3-dimethylbutyl)-4-oxothiazolidin-5-yl)acetic acid as a yellow gum which was carried on to the next step as is. LC/MS: 468.39 (M+1) Rt=diastereomers at 1.91 and 1.93 min (10-90% 3/5 min (grad/run) w/formic acid).

1. customVolatiles were removed on a rotary evaporator under high vacuum