51255-17-5Relevant articles and documents
Preparation method of decitabine intermediate
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Paragraph 0043-0045, (2020/07/24)
The invention belongs to the field of pharmaceutical synthesis, and discloses a preparation method and a purification method of a decitabine intermediate (V). The preparation method comprises the following steps of enabling 2-deoxygenation-D-ribose derivative (III) and hexamethyldisilazane-activated 5-azacytosine (IV) to be subjected to a coupling reaction under the action of a catalyst to be purified to obtain the decitabine intermediate (V). The method is simple and convenient to operate, no silica gel column purification product is needed, and the method is suitable for industrial production.
The development of β-selective glycosylation reactions with benzyl substituted 2-deoxy-1,4-dithio-D-erythro-pentofuranosides: enabling practical multi-gram syntheses of 4'-Thio-2'-deoxycytidine (T-dCyd) and 5-aza-4’-thio-2’-deoxycytidine (aza-T-dCyd) to s
Wishka, Donn G.,Lopez, Omar D.,Rudchenko, Vladimir F.,Huang, Guangfei,Bahde, Robert,Kumar, Vineet,Denysenko, Sergiy M.,Zhang, Lianhao,Zhang, Mianji,Teicher, Beverly A.,Morris, Joel
, p. 68 - 95 (2020/10/21)
The lack of effective methods to perform direct β-selective glycosylation reactions with 2-deoxy-1,4-dithio-D-erythro-pentofuranosides has long been a significant stumbling block for the multi-gram synthesis of 4’-thio-2’-deoxy nucleosides. In addition, p
Purification method of decitabine intermediate
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Paragraph 0038; 0039, (2020/07/24)
The invention belongs to the technical field of medicinal chemistry, and particularly relates to a purification method of a decitabine intermediate. The method comprises the following steps: dissolving a decitabine intermediate crude product in a first solvent such as trichloromethane, and adding a second solvent such as methyl tert-butyl ether, so that impurities generated in the synthesis process can be effectively removed, and the proportion of beta-configuration products can be increased when the refined intermediate is subjected to a glycosylation reaction.