反应详情

To (R)-3-methyl-5-(2-(4-methylthiazol-2-yl)pyrrolidine-1-carbonyl)benzoic acid (330 mg, 1 mmol) in CH2Cl2 at rt, EDCI (269 mg, 1.4 mmol) and HOBT (162 mg, 1.20 mmol) were added and stirred at rt for 20 min. In a separate flask (2R,3S)-3-amino-4-phenyl-1-(3-(trifluoromethyl)benzylamino)butan-2-ol was taken in CH2Cl2 and treated with DIPEA (2 ml). After 20 min, flask containing acid was cooled to 0° C. and the amine was added to it. Reaction mixture was stirred at rt for 16 h. Then reaction mixture was diluted with ethyl acetate, washed with sodium bicarbonate, water, brine and dried. Crude residue was purified by column chromatography to yield 60% of desired product.

1. waitAfter 20 min
2. additionflask containing acid
3. temperaturewas cooled to 0° C.
4. customReaction mixture
5. stirringwas stirred at rt for 16 h
6. customThen reaction mixture
7. washwashed with sodium bicarbonate, water, brine
8. customdried
9. customCrude residue was purified by column chromatography