- Preparation method of beta-configuration gemcitabine hydrochloride intermediate
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The invention provides a preparation method of a beta-configuration gemcitabine hydrochloride intermediate, which comprises the following step: in a solvent, in the presence of an alpha-configurationgemcitabine hydrochloride intermediate II', reacting a gemcitabine hydrochloride intermediate I with silanized cytosine to prepare the beta-configuration gemcitabine hydrochloride intermediate II. Thebeta-configuration gemcitabine hydrochloride intermediate II is prepared in the presence of the alpha-configuration gemcitabine hydrochloride intermediate II', and the production of the alpha-configuration gemcitabine hydrochloride intermediate is effectively inhibited, so that the yield and the purity of a target product, namely the beta-configuration gemcitabine hydrochloride intermediate II, are improved, and post-treatment steps are simplified.
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Paragraph 0028; 0036-0054
(2021/04/01)
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- Industrial preparation process for key intermediate sulfonated saccharide of Gemcitabine
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The invention relates to a preparation method for a compound represented by a formula (I) shown in the description, i.e., a key intermediate sulfonated saccharide of Gemcitabine. The final product is prepared through subjecting a compound represented by a formula (II) shown in the description to sodium borohydride reduction, hydroxyl protection and resolution. The method is simple in process, high in yield and high in product purity and has no need of harsh reaction conditions, thereby being very suitable for industrial production.
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- A miazines new compounds
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The invention relates to a new pyrimidine compound. The experiment proves that the new compound disclosed in the specification can inhibit growth of tumor cells, and has favorable effectiveness and safety when being used for preparing antineoplastic drugs. The vessel irritation experiment proves that the new compound does not have hemolysis or irritation and can be prepared into an injection for clinical use.
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Paragraph 0007; 0010; 0011
(2017/07/07)
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- Preparation method of difluoro nucleoside anticancer drugs capable of destroying cell replication
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The invention relates to a preparation method of difluoro nucleoside anticancer drugs capable of destroying cell replication. The preparation method comprises steps as follows: cytosine is taken as a raw material and subjected to a reaction with hexamethyl disilazane, a silyl ether protecting group is generated and docked with 2-deoxy-2,2-difluoro-D-erythro-pentofuranose-3,5-dibenzoate-1-methanesulfonate, and a final product is obtained after post-processing with hydrochloric acid. According to the method, the technology is simple, the operating condition is more convenient, the generation proportion of required isomers is high, the solvent is environment-friendly, harsh reaction conditions are not needed, and the method is suitable for industrial production.
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Paragraph 0023; 0024
(2016/11/24)
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- Stereospecific synthesis of 2-deoxy-2,2-difluororibonolactone and its use in the preparation of 2'-deoxy-2',2'-difluoro-β-D-ribofuranosyl pyrimidine nucleosides: The key role of selective crystallization
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A stereospecific synthesis of 2'-deoxy-2',2'-difluorocytidine (gemcitabine), a potential anticancer agent, is described. The stereoselectivity was accomplished via two diastereoselective crystallizations, i.e. the crystallization of the key intermediate, difluororibonolactone 2a, and the crystallization of the hydrochloride salt of gemcitabine 16b from the anomeric mixture. Because of the availability of 2a in large quantities, other 2'-deoxy-2',2'-difluoropyrimidine nucleosides such as 2'-deoxy-2',2'-difluorouridine (19) were synthesized for structure-activity relationship studies.
- Chou,Heath,Patterson,Poteet,Lakin,Hunt
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p. 565 - 570
(2007/10/02)
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