Synthesis method of beta-thymidine
A synthetic method and technology of thymidine, applied in the field of β-thymidine synthesis, can solve the problems of cumbersome post-processing remedial operations, low purity of target products, unstable intermediate compounds, etc., to achieve large-scale promotion and results Stable and less polluting effect
Active Publication Date: 2017-06-13
抚州市星辰药业有限公司
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Problems solved by technology
However, most of the methods for β-thymidine synthesized by the thymine method currently have unstable intermediate compounds, and the target product is not pure enough to be easily decomposed in the follow-up process. Development of Zidovudine Industrialized Production
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[0033] The present invention will be further described below in conjunction with the examples. It should be understood that these examples are only for the purpose of illustration, and in no way limit the protection scope of the present invention.
[0034] A kind of synthetic method of β-thymidine, its technological process is specifically as follows:
[0035] 1. Add 900kg of trimethylaluminum silane and 500kg of 5-methyluracil to a 2000L glass-lined reactor at one time, open the steam heating valve, raise the temperature to 80°C, and reflux for 20 hours. The exhaust gas generated during the reaction was absorbed with a potassium hydroxide solution with a mass fraction of 48%. Trimethylchlorosilane is recovered by distillation for recycling, and the residue is transferred to the next reaction kettle. The distillation residue is mainly compound A, and the chemical structural formula of compound A is:
[0036]
[0037] The main reaction formula of step 1 is:
[0038]
[...
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The invention discloses a synthesis method of beta-thymidine. The synthesis method takes trimethylchlorosilane and 5-methyluracil as raw materials to react; in a reaction line process, tetraacetylribose, trifluoromethanesulfonic acid, N,N-dimethylformamide and acetylchloride are introduced; then hydrogenation reaction and hydrolysis reaction are carried out to finally obtain a beta-thymidine finished product and the yield is 89 percent. Compared with an existing synthesis method, the synthesis method of the beta-thymidine has the advantages that the price of raw materials is low, the content of the beta-thymidine in the final product is high, and pollution to the environment in a production process is small; in a synthesis process, the content of generated impurities is less. According to the synthesis method disclosed by the invention, an obtained result is stable and the operation is simple; demands on equipment and preparation environments are not strict so that large-scale popularization is facilitated.
Description
technical field [0001] The invention belongs to the field of medical drugs, in particular to a method for synthesizing β-thymidine. Background technique [0002] As one of the important raw materials for the synthesis of stavudine, β-thymidine is an important pharmaceutical intermediate with good antiviral effects and significant effects in cancer chemotherapy and antiviral aspects. The important raw material of Fuding. β-thymidine, also known as thymidine, is the abbreviation of thymidine deoxynucleoside. Its chemical name is 1-(2′-deoxy-β-D-ribofuranose)-5-methyluridine, and its English name is Thymidine. Molecular formula is C 10 h 14 N 2 o 5 , the molecular weight is 242.2286, the CAS registration number is 50-89-5, and the structural formula is: [0003] [0004] There is no natural product of β-thymidine. At present, the main preparation methods include chemical synthesis, DNA enzymatic hydrolysis, fermentation, etc. The biological method requires high product...
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IPC IPC(8): C07H19/073C07H1/00
CPCC07H1/00C07H19/073
Inventor 陈红斌黄素玉
Owner 抚州市星辰药业有限公司