abstract |
The invention relates to a synthetic method of Tegoprazan and analogues thereof. The method involves the reaction of a 4-halo-2-methyl-1H-benzo [d] imidazole-6-carboxylate or 4-halo-2-methyl-1H-benzo [d] imidazole-6-carboxylic acid amide compound with (S) -5, 7-difluoro-3, 4-dihydro-2H-chromene-4-ol in the presence of copper reagent/base/additive/solvent, to prepare 4-[ ( (4S) -5, 7-difluoro-3, 4-2H-chromenen-4-yl) oxy] -2-methyl-1H-benzo [d] imidazole-6-carbox ylate or 4-[ ( (4S) -5, 7-difluoro-3, 4-2H-chromenen-4-yl) oxy] -2-methyl-1H-benzo [d] imidazole-6-carbox ylic acid amide. |