反应详情

1,4,6,7-Tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester (0.70 g, 3.1 mmol) was dissolved in trifluoroacetic acid (10 mL) at 0° C., stirred for 1 h, and was concentrated. The residue was dissolved in ethanol and treated with concentrated hydrochloric acid (1 mL). The bis-hydrochloride salt precipitated out as a white solid which was filtered to give 510 mg (83%). The free base was prepared as needed by dissolving the salt in water, loading it onto an SCX column, flushing with methanol, and then eluting with 2 M ammonia in methanol.

1. concentrationwas concentrated
2. dissolutionThe residue was dissolved in ethanol
3. additiontreated with concentrated hydrochloric acid (1 mL)
4. customThe bis-hydrochloride salt precipitated out as a white solid which
5. filtrationwas filtered
6. customto give 510 mg (83%)
7. customThe free base was prepared
8. customflushing with methanol
9. washeluting with 2 M ammonia in methanol