134790-39-9Relevant articles and documents
Preparation method of beta-configuration gemcitabine hydrochloride intermediate
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Paragraph 0028; 0036-0054, (2021/04/01)
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.
A miazines new compounds
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Paragraph 0007; 0010; 0011, (2017/07/07)
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.
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
Chou,Heath,Patterson,Poteet,Lakin,Hunt
, p. 565 - 570 (2007/10/02)
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.