反应详情

温度

170 °C

4-Chloro-2-(4-fluorophenyl)-1H-pyrrolo[2,3-b]pyridine-5-carbonitrile (30 mg, 0.11 mmol), N-(3-aminomethylpyridin-2-yl)-N-methylmethanesulfonamide (159 mg, 0.552 mmol) and N-ethyldiisopropylamine (0.282 ml, 1.656 mmol) are suspended in 0.4 ml of 1-methyl-2-pyrrolidone and heated in a microwave at 170° C. for 40 min. The reaction is still not complete even after a further 40 min, so that a further equivalent of N-(3-aminomethylpyridin-2-yl)-N-methylmethanesulfonamide (31.8 mg, 0.110 mmol) is added, and the batch is heated at 170° C. for a further 60 min. For work-up, the batch is partitioned between water and ethyl acetate, the organic phase is dried (Na2SO4) and evaporated, giving a brown oil, which is purified by chromatography; yield: 17 mg (34%); LC-MS: 451 [M+H]+; HPLC: 3.07 (RT/min).

1. additionis added
2. temperaturethe batch is heated at 170° C. for a further 60 min
3. customFor work-up, the batch is partitioned between water and ethyl acetate
4. dry with materialthe organic phase is dried (Na2SO4)
5. customevaporated
6. customgiving a brown oil, which
7. customis purified by chromatography
8. custom3.07 (RT/min)