Pyridine → HCID 136381716, compound

Participants

Reaction Conditions

Reaction Steps

(E)-2-[2-(1H-indazol-3-yl)vinyl]-N-hydroxybenzamidine (0.06 g, 0.22 mmol) obtained in Step 1 of Example 175 was dissolved in DMF (1.0 mL), and pyridine (35 μL, 0.43 mmol) and ethylchloroformate (0.12 mL, 1.1 mmol) were added thereto, followed by stirring at 0° C. for 30 minutes. The mixture was added with water and the precipitated solid was collected by filtration and the solid was dried. The obtained solid was dissolved in toluene (2.0 mL) at 0° C. and added with potassium tert-butoxide (85 mg, 0.76 mmol), followed by stirring at 60° C. for 2 hours. Then, the mixture was neutralized using aqueous fumaric acid solution. The reaction mixture was extracted with ethyl acetate and the organic layer was concentrated. The residue was triturated in a mixed solvent of ethyl acetate/hexane to obtain Compound 178 (18 mg, 23%).

Provenance & Evidence