反应详情

The subtitle compound was prepared analogous to the method described in Example 19 (step 19a). A mixture of (1R,2S)-2-amino-1-(3-ethylphenyl)propan-1-ol hydrochloride (22b, 216 mg, 1.00 mmol), 1-(4-fluorophenyl)-5-iodo-1H-indazole (406 mg, 1.20 mmol), cesium carbonate (979 mg, 3.00 mmol) and copper(I) iodide (38.1 mg, 0.20 mmol) in butyronitrile (3 mL) was heated for 19 h at +125° C. in a sealed reactiontube flushed with Argon. After final purification by HPLC the obtained material was dissolved in tert-Butyl methyl ether, and precipitated as the hydrochloride salt by adding a solution of 6-7 N HCl in 2-propanol. Yield 199 mg (46%)

1. temperaturewas heated for 19 h at +125° C. in a sealed reactiontube
2. customflushed with Argon
3. customAfter final purification by HPLC the obtained material
4. dissolutionwas dissolved in tert-Butyl methyl ether
5. customprecipitated as the hydrochloride salt
6. additionby adding a solution of 6-7 N HCl in 2-propanol