反应详情

温度

110 °C

A mixture of 2-bromo-5-[2-(4-cyclobutylpiperazin-1-yl)-2-oxoethyl]-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine (40 mg, 0.1 mmol), 3-methylsulfonyl-phenylboronic acid (40 mg, 0.2 mmol), Na2CO3 (42 mg, 0.4 mmol) and Pd(PPh3)4 (12 mg, 0.01 mmol) in DME (4 mL) and water (1 mL) is degassed with argon and heated at 110° C. in a sealed tube overnight. The mixture is cooled and the layers are separated. The aqueous layer is extracted with EtOAc (4 ml) and the combined extracts are dried and evaporated. The residue is purified by PTLC to give the title compound as a white solid. MS (M+1): 475.0; 1H NMR (δ, CDCl3): 8.44 (t, 1H), 8.15 (td, 1H), 7.94 (td, 1H), 7.62 (t, 1H), 3.86 (s, 2H), 3.65 (q, 4H), 3.46 (d, 2H), 3.09 (s, 2H), 2.97 (s, 3H), 2.68-2.78 (m, 1H), 2.33 (q, 4H), 1.62-2.07 (m, 6H).

1. customis degassed with argon
2. temperatureThe mixture is cooled
3. customthe layers are separated
4. extractionThe aqueous layer is extracted with EtOAc (4 ml)
5. customthe combined extracts are dried
6. customevaporated
7. customThe residue is purified by PTLC