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Tipiracil intermediate compound
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A technology for tipiracil and intermediates, applied in the field of drug synthesis, can solve the problems of difficult to pass the target product and low yield, and achieve the effect of being suitable for industrial production, easy to operate, and improving safety
Pending Publication Date: 2020-12-04
LUNAN PHARMA GROUP CORPORATION
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[0022] In summary, in the reported technical methods for preparing tipiracil, the main problem is that the target product is easily hydrolyzed to produce impurity D, which makes the target product difficult to pass, or the yield is low after repeated refining
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Embodiment 1
[0065] Add SM-1 (9.75g, 50mmol) and SM-2 (18.30g, 62.5mmol) into methanol (80mL), until the materials are completely dissolved, add dropwise a solution of DBU (24.36g, 160mmol) dissolved in methanol (30mL) , the dropwise addition is completed, the temperature is controlled at 45-50°C for 14 hours, the reaction solution is filtered while it is hot, the filtrate is cooled to 0-5°C, stirred and crystallized for 2-3 hours, filtered with suction, and the obtained filter cake is vacuum-dried to obtain the pyrazidine intermediate Compound I, yield 93.5%, purity 99.88%.
Embodiment 2
[0067] Add SM-1 (9.75g, 50mmol) and SM-2 (16.10g, 55.0mmol) into methanol (80mL), until the materials are completely dissolved, add dropwise a solution of DBU (30.45g, 200mmol) dissolved in methanol (30mL) , the dropwise addition is completed, the temperature is controlled at 45-50°C for 14 hours, the reaction solution is filtered while it is hot, the filtrate is cooled to 0-5°C, stirred and crystallized for 2-3 hours, filtered with suction, and the obtained filter cake is vacuum-dried to obtain the pyrazidine intermediate Compound I, yield 90.8%, purity 99.75%.
Embodiment 3
[0069] Add SM-1 (9.75g, 50mmol) and SM-2 (20.50g, 70mmol) in methanol (80mL), until the materials are completely dissolved, add dropwise a solution of DBU (19.03g, 125mmol) dissolved in methanol (30mL), After the dropwise addition is completed, the temperature is controlled at 45-50°C for 14 hours, the reaction solution is filtered while it is hot, the filtrate is cooled to 0-5°C, stirred and crystallized for 2-3 hours, filtered with suction, and the obtained filter cake is vacuum-dried to obtain pyrazidine intermediate I The compound has a yield of 90.5% and a purity of 99.73%.
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Abstract
The invention belongs to the technical field of medicine synthesis, and particularly relates to a tipiracil intermediate compound. The synthesis method of the tipiracil intermediate compound comprisesthe following steps: adding SM-1 and SM-2 into an organic solvent, dropwise adding an alkaline solution into a reaction solution, carrying out a temperature-controlled reaction, and filtering to obtain a tipiracil intermediate compound I. The preparation method of the compound is mild in reaction condition, simple in operation process and low in production cost, and the tipiracil prepared from the compound has high purity and yield, and is suitable for industrial production.
Description
technical field [0001] The invention belongs to the field of drug synthesis, in particular to a tipiracil intermediate compound. Background technique [0002] Colorectal cancer (CRC), including colon cancer and rectal cancer, is one of the most common malignant tumors, and its morbidity and mortality rank third among digestive tract malignancies after gastric cancer and esophageal cancer. China is a low-incidence area in the world, but the incidence of colorectal cancer in my country has shown an obvious upward trend in recent years, and it has become one of the fastest-rising malignant tumors in my country. [0003] Due to the lack of obvious early symptoms of colorectal cancer and the lack of early screening measures, most patients have developed to the middle and late stages when they see a doctor. For the treatment of advanced colorectal cancer, the first choice is medical treatment based on chemotherapy. Among them, the new drug Lonsurf (trifluridine (FTD) / hydrochlori...
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