反应详情

An additional approach to compounds such as x is outlined in Scheme 4. Treatment of an appropriate alcohol R5—OH and a base such as NaH and the like, followed by addition of xvii will provide the ether xviii. The bromide xviii can be converted into the methylated intermediate xix via palladium-mediated cross coupling with Me3B3O3 and the like. The nitro derivative xix can be treated with Pd/C in the presence of HCOONH4 to produce the amine xx. The amine xx can be acylated to provide xxi. The acylated amine xxi can be treated with iso-amyl nitrate in the presence of Ac2O/KOAc and the like to provide the N-acyl indazole xxii. Compounds such as xxii can be treated with ammonia and the like to produce indazoles xxi. The indazole xxi can be treated with iodine and KOH and the like to provide the iodo-indazole xxii. The indazole nitrogen can be protected with trityl chloride and base and the like to provide xxiii. The iodo-indazole xxiii can be converted into xxiv via cross coupling using the appropriate boronic acid and the like and an appropriate palladium catalyst. The chloro-pyridine xxiv can be converted into examples such as x using the appropriate amine (HN(R2)R3), palladium catalyst, and ligand followed by deprotection of the trityl group using standard conditions.