Synthesis of amlodipine besylate to achieve room temperature operation The "Amlodipine besylate tablet research" undertaken by Tianjin Pharmaceutical Research Institute recently won the third prize of the 2005 Tianjin Science and Technology Progress Award. In the study of the synthesis process, the researchers of the institute chose phthalic anhydride and ethanolamine as the starting materials, and synthesized amlodipine besylate through the steps of acylation, hydrocarbonation, condensation, and hydrazinolysis. Through a lot of literature research and repeated experiments, scientific researchers have overcome the problem of low-temperature reaction operation technology. After improvement, the reaction conditions have changed from minus 10 ℃ to room temperature operation, and the yield has been increased from 80% to 90%; Problem, the structure and source of the main impurities were determined through separation and identification. Amlodipine besylate has a half-life of 36 hours and is well tolerated. Oral administration once a day can continue to lower blood pressure for 24 hours. The successful development of this product provides a better treatment option for the majority of patients with hypertension and angina pectoris, and the product technology has reached the domestic advanced level.
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