4-Chloro-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine is used in the design and preparation of ruxolitinib.
4-chloro-7-(((2-(trimethylsilyl) ethoxy) methyl)-7h-pyrrolo [2,3-d] pyrimidine, an organic intermediate, can be prepared from 4-chloropyrrolopyrimidine and 2-(trimethylsilyl) ethoxymethyl chloride prepared by one-step reaction, alkali can be selected from sodium hydrogen, can be used as organic synthesis intermediates and pharmaceutical intermediates, mainly used in laboratory research and development process and chemical production process.
Add 450g 4-chloropyrrolo [2,3-d] pyrimidine to 3.6L DMF, the temperature was cooled to -10 °c to -20 °c, and 144g of sodium hydride (60%) was added in portions. 586.0G 2-(trimethylsilyl) ethoxymethyl chloride was slowly added dropwise, and the reaction was stirred for 2 hours. After completion of the reaction, 36g of glacial acetic acid was added dropwise with stirring to quench the reaction. The reaction solution was poured into 14.4L of purified water, extracted with ethyl acetate, and washed with saturated brine. The organic layer was concentrated under reduced pressure to remove the solvent, and the residue was purified by 200-300 mesh silica gel column chromatography to obtain 4-chloro-7-((2-(trimethylsilyl) ethoxy) methyl)-7h-pyrrolo [2,3-d] pyrimidine (808.2g,97.2%).
