反应详情

温度

0 °C

N-[6-[5-Amino-6-(methyloxy)-3-pyridinyl]-2-(tetrahydro-2H-pyran-2-yl)-2H-indazol-4-yl]-2-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-thiazole-4-carboxamide (250 mg) was dissolved in DCM (6 ml) and N-methylmorpholine (0.143 ml) was added. The reaction was cooled to 0° C. in an ice bath, then 2-chloroethanesulfonyl chloride (0.047 ml) was added dropwise. The reaction was left to warm to RT overnight. Reaction had blown dry, so was redissolved in DCM (6 ml). Further 2-chloroethanesulfonyl chloride (0.047 ml) was added and stirred at RT for 2 hours. Water (6 ml) was added to the reaction. The DCM was separated, passed through a hydrophobic frit, then evaporated to dryness to give crude title compound (250 mg) used directly in the next step without further purification.

1. waitThe reaction was left
2. temperatureto warm to RT overnight
3. customReaction
4. customhad blown dry
5. dissolutionso was redissolved in DCM (6 ml)
6. additionFurther 2-chloroethanesulfonyl chloride (0.047 ml) was added
7. additionWater (6 ml) was added to the reaction
8. customThe DCM was separated
9. customevaporated to dryness