反应详情

A mixture of {2-[2-cyclopentyl-1-(4-methanesulfonyl-phenyl)-ethyl]-1H-pyrrolo[2,3-b]pyridin-5-yl}-acetonitrile (as prepared in Example 38, 140 mg, 0.34 mmol) in 36% hydrochloric acid (1 mL) and acetic acid (5 mL) was refluxed for 2 h. The mixture was concentrated in vacuo, extracted with ethyl acetate (250 mL), washed with brine, dried over anhydrous sodium sulfate and then concentrated in vacuo to afford {2-[2-cyclopentyl-1-(4-methanesulfonyl-phenyl)-ethyl]-1H-pyrrolo[2,3-b]pyridin-5-yl}-acetic acid (150 mg, quant.) as a light yellow solid which was used in the next step without further purification: LC/MS m/e calcd for C23H2N2O4S [M+H]+ 427.54, observed 427.0.

1. temperaturewas refluxed for 2 h
2. concentrationThe mixture was concentrated in vacuo
3. extractionextracted with ethyl acetate (250 mL)
4. washwashed with brine
5. dry with materialdried over anhydrous sodium sulfate
6. concentrationconcentrated in vacuo