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Preparation method of ambrisentan
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Paragraph 0048-0052, (2019/05/15)
The invention belongs to the field of medicine synthesis and particularly relates to a preparation method of ambrisentan, wherein the ambrisentan is prepared through a benzyl protection reaction, a condensation reaction, and a benzyl protection group removal reaction in the method. A benzyl-protected intermediate is delivered to the next step of the condensation reaction without post-treatment. The debenzylation reaction is carried out through catalytic hydrogenation, which is green and environment-friendly and is simple in reaction operations and post-treatment. A reaction liquid is treated and pulped in an ether solvent, so that residual raw materials and intermediate in the solid are removed effectively. When an ambrisentan crude product is prepared, a recrystallization step with a methanol/water mixed solvent is carried out to obtain high-purity ambrisentan. The method is fewer in steps and high in yield, has short production cycle, simple operation, good reproducibility and mild conditions, and is suitable for industrial production.
