反应详情

温度

100 °C

(R)-3-(3-Bromo-4-methyl-benzoylamino)-4-(2-chloro-phenyl)-butyric acid ethyl ester (103 mg, 235 μmol, 1.0 eq.) was combined with 2-t-butoxycarbonylphenylboronic acid pinacol ester (85.9 mg, 282 μmol, 1.2 eq.). Toluene (328 μL) was added followed by EtOH (180 μL) then K2CO3 (65.1 mg, 471 μmol, 2.0 eq.) predissolved in water (61.5 μL). The mixture was stirred to aid in dissolution. The reaction vessel was purged with nitrogen then Pd(PPh3)4 (27.2 mg, 23.5 μmol) was added quickly. The reaction vessel was capped and heated to 100° C. for 30 minutes. The organics were removed and evaporated under vacuum. 1:1 TFA/DCM (0.2 mL each) was added and the resulting mixture was stirred for 30 minutes. The solvents were evaporated and THF (3 mL) and 1 M aqueous NaOH (706 μL, 3.0 eq.) were added. The mixture was stirred for 2 hours and EtOAc was added.

1. dissolutionto aid in dissolution
2. customThe reaction vessel was purged with nitrogen
3. customThe reaction vessel was capped
4. customThe organics were removed
5. customevaporated under vacuum
6. addition1:1 TFA/DCM (0.2 mL each) was added
7. stirringthe resulting mixture was stirred for 30 minutes
8. customThe solvents were evaporated
9. stirringThe mixture was stirred for 2 hours