反应详情

温度

85 °C

To a sealed tube containing 2-[5-bromo-1-(cyclopropylmethyl)-1H-indol-3-yl]acetic acid (100 mg, 0.32 mmol), 2-thiopheneboronic acid (124 mg, 0.97 mmol), (C6H5)4Pd (37 mg, 0.032 mmol), Na2CO3 (2.6 mmol) in a mixture of benzene/EtOH/H2O (5/1/3, 4.5 mL) was heated at 85° C. for 19 h. The mixture was poured onto diethyl ether and adjusted to pH 3 before extracting with diethyl ether. The mixture was washed with NaH2PO4, dried over MgSO4 and evaporated to give the crude product which was purified on silica gel column (33% EtOAc in hexane with 1% HCOOH) to give 79 mg (78% yield) of the product.

1. additionThe mixture was poured onto diethyl ether
2. extractionbefore extracting with diethyl ether
3. washThe mixture was washed with NaH2PO4
4. dry with materialdried over MgSO4
5. customevaporated
6. customto give the crude product which
7. customwas purified on silica gel column (33% EtOAc in hexane with 1% HCOOH)