反应详情

2-(3-Carboxy-propyl)benzoic acid (160 mg, 790 μmol, 1.0 eq.), DIPEA (439 μL, 3.2 eq.) and HATU (300 mg, 788 μmol, 1.0 eq.) were combined in DCM (20 mL) and stirred for 5 minutes at room temperature. (R)-3-amino-4-(2-chloro-phenyl)-butyric acid ethyl ester (200 mg, 827 μmol, 1.1 eq.) was added and the resulting mixture was stirred for 1 hour. The reaction was quenched with saturated NH4Cl, and the product was extracted with DCM, dried and evaporated. THF (20 mL) and 10 M aqueous NaOH (315 μL) was added and the mixture was stirred for 1 hour. The crude material was dissolved in AcOH (1.5 mL) and purified using preparative HPLC to yield the title compound (25 mg, 95% purity). MS m/z [M+H]+ calc'd for C21H22ClNO5, 404.12. found 404.4.

1. stirringthe resulting mixture was stirred for 1 hour
2. customThe reaction was quenched with saturated NH4Cl
3. extractionthe product was extracted with DCM
4. customdried
5. customevaporated
6. additionTHF (20 mL) and 10 M aqueous NaOH (315 μL) was added
7. stirringthe mixture was stirred for 1 hour
8. dissolutionThe crude material was dissolved in AcOH (1.5 mL)
9. custompurified