Green method for synthesizing AE-active ester through microwave-assisted process

• Main Authors: FANG ZHENGWEI, MENG XIANQIANG, YU FUGANG, JIA KAILEI
• Format: Patent
• Language: Chinese; English
• Published: 21.12.2018
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention belongs to the technical field of synthesis of medicines and particularly relates to a green method for synthesizing AE-active ester through a microwave-assisted process. The green method for synthesizing AE-active ester through the microwave-assisted process comprises the following steps: firstly adding 2-(2-aminothiazole-4-yl)-2-methoxyiminoacetic acid, dithiodibenzothiazole, catalyst and solvent into a microwave reactor, then dropwise adding triethyl phosphate into the microwave reactor, reacting, carrying out suction filtration and recrystallization to obtain a product. The synthesis method is simple to operate and low in cost; the productivity can be greatly improved; the yield is increased and reaches up to 95%; the purity of the product is relatively high and reaches over 99%; the pleasantly surprised technical effect can be obtained. 本发明属于医药合成技术领域，具体涉及种微波辅助法合成AE-活性酯的绿色工艺。所述的微波辅助法合成AE-活性酯的绿色工艺，包括以下步骤：首先，将氨噻肟酸、二硫代二苯并噻唑、催化剂、溶剂加入到微波反应器中，然后，向内滴加亚磷酸三乙酯反应，抽滤，重结晶，得产品。本发明的合成方法，操作简单，成本低，产能大幅度提高，收率