1234208-67-3Relevant academic research and scientific papers
For the preparation of (2 - methyl - 1 - (3 - methyl benzyl) - 1H - benzo [d] imidazol - 5 - yl) (piperidin - 5 - yl) methanone method
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, (2017/08/25)
The present invention relates to a method for preparing (2-methyl-1-(3-methylbenzyl)-1H-benzo[d]imidazol-1-yl)(piperidin-5-yl)methanone having an activity as a protease activated receptor-2 (PAR-2) inhibitor, and an intermediate thereof. When (2-methyl-1-(3-methylbenzyl)-1H-benzo[d]imidazol-1-yl)(piperidin-5-yl)methanone represented by chemical formula 1, which has an activity as a PAR-2 inhibitor and can be used for treating and preventing inflammatory diseases, is prepared using an amine compound as a novel intermediate compound according to the present invention, the reaction steps are reduced as a whole, costs are saved, crystallization is effective and the total yield is increased since the introduction of a protecting group and the reaction of a deprotecting group are unnecessary. In addition, with respect to separation and purification of the compound represented by chemical formula 1, which is a final product, a crystallization method, an extraction method and the like suitable for industrial-sized synthesis can be used, thereby being very economical.
