An optimized multi-step synthesis of a new highly effective and low-toxicity derivative of o-benzoylaminobenzoic acid amides possessing anxiolytic activity is presented. Anthranylamide and propionic anhydride instead of acetic anhydride were used as starting materials. The number of synthetic steps did not increase as compared to the known method because the hydrolysis of anthranylamide proceeded in an alkaline medium, in which the Schotten–Bauman acylation was carried out. The preparation of 2-benzoylamino-N-[4-(4,6-dimethylpyrimidin-2-ylsulfamoyl)phenyl]benzamide in the final step was modified by replacing the polar aprotic solvent DMF by the less toxic and more environmentally friendly DMSO. Use of more accessible and cost-effective starting materials in combination with Schotten–Bauman acylation, which eliminated environmentally hazardous benzene, was advisable for production of the active pharmaceutical ingredient. The developed laboratory procedure could be successfully used to obtain other biologically active compounds of o-benzoylaminobenzoic acid and their cyclic derivatives.

提出了一种具有抗焦虑活性的新型高效低毒邻苯甲酰氨基苯甲酰胺衍生物的优化多步合成。使用邻氨基苯甲酰胺和丙酸酐代替乙酸酐作为原料。与已知方法相比，合成步骤的数量没有增加，因为邻氨基苯甲酰胺的水解是在碱性介质中进行的，其中进行了 Schotten-Bauman 酰化。2-苯甲酰氨基-N的制备-[4-(4,6-二甲基嘧啶-2-基氨磺酰基)苯基]苯甲酰胺在最后一步通过用毒性更小、更环保的DMSO代替极性非质子溶剂DMF进行改性。使用更容易获得且更具成本效益的起始材料与 Schotten-Bauman 酰化相结合，消除了对环境有害的苯，对于活性药物成分的生产是可取的。开发的实验室程序可成功用于获得邻苯甲酰氨基苯甲酸及其环状衍生物的其他生物活性化合物。