Thionyl Chloride → HCID 86639153, compound

Participants

Reaction Steps

Thionyl chloride (230 μL) and the intermediate synthesized in Example 151, (S)-4-[4-(2-ethyl-2H-pyrazol-3-ylamino)phenyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-acetic acid (500 mg), were successively added to methoxy ethanol (10 mL) at 0° C., and the mixture was stirred at room temperature for 1 day. After completion of the reaction, the mixture was partitioned by adding water and ethyl acetate. The organic layer was washed with aqueous sodium hydrogencarbonate, and the solvent was evaporated. The residue was purified by column chromatography (chloroform:methanol=100:1) to give the title compound (410 mg).

Provenance & Evidence