反应详情

2-(3-Carboxy-propyl)benzoic acid (300 mg, 1.4 mmol, 1.0 eq.) was combined with DIPEA (803 μL, 3.2 eq.) and HATU (548 mg, 1.4 mmol, 1.0 eq.) in DCM (30 mL). The mixture was stirred for 10 min and (2R,3R)-3-amino-4-(2-chloro-phenyl)-2-hydroxy-butyric acid butyl ester (412 mg, 1.4 mmol, 1.0 eq.) was added. The reaction was quenched after 1 hour by adding saturated NH4Cl and the product was extracted with DCM, dried and evaporated. AcOH (1 mL) was added and the resulting product was purified by preparative HPLC to yield the title compound (260 mg, 99% purity). MS m/z [M+H]+ calc'd for C25H30ClNO6, 476.18. found 476.2.

1. customThe reaction was quenched after 1 hour
2. additionby adding saturated NH4Cl
3. extractionthe product was extracted with DCM
4. customdried
5. customevaporated
6. additionAcOH (1 mL) was added
7. customthe resulting product was purified by preparative HPLC