反应详情

温度

100 °C

A mixture of 2,3-dichloro-4-iodo-furo[2,3-c]pyridin-7-ylamine (300.0 mg, 0.9121 mmol), 4-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-pyrazol-1-yl]-piperidine-1-carboxylic acid tert-butyl ester (516 mg, 1.37 mmol) and Pd(PPh3)4 (50 mg, 0.04 mmol) in 1,4-dioxane (20 mL) and H2O (2 mL) was degassed and refilled with argon (3×). The reaction was heated at 100° C. for 20 h using a Biotage Initiator microwave reactor. The reaction was concentrated in vacuo to give a solid which was purified by flash chromatography (30 to 60% EtOAc:hexanes), which afforded the desired intermediate. 1H NMR (400 MHz, CDCl3): δ 7.85 (s, 1H), 7.65 (s, 1H), 7.57 (s, 1H), 4.80 (br s, 2H), 4.32 (m, 3H), 2.99 (m, 2H), 2.18 (m, 2H), 1.97 (m, 2H), 1.47 (s, 9H); MS (ESI): 452.00 [M+H]+; HPLC tR=3.14 min.

1. customwas degassed
2. additionrefilled with argon (3×)
3. concentrationThe reaction was concentrated in vacuo
4. customto give a solid which
5. customwas purified by flash chromatography (30 to 60% EtOAc:hexanes), which