2328091-01-4Relevant articles and documents
Preparation method of Remdesivir
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Paragraph 0039; 0041-0043, (2020/06/16)
The invention relates to a preparation method of Remdesivir. 4-amino-7-bromopyrrolo [2, 1-f][1, 2, 4] triazine and (3alpha R, 6R, 6alpha R)-6-(benzyloxymethyl)-2, 2-dimethyl dihydrofuran [3, 4-d] [1,3] dioxo-4 (4alpha H)-one are taken as a raw material, amino protection reaction, coupling reaction, substitution reaction, debenzylation reaction, resolution, alcoholysis reaction, amidation reaction, deprotection reaction and resolution nine reaction steps are carried out so as to synthesize Remdesivir at a high yield. The preparation method of Remdesivir provided by the invention is a preparation method which is high in yield, low in cost, easy to operate and suitable for industrialization.
2'-C-methyl-substituted nucleoside compound and preparing method and application thereof
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Paragraph 0298-0302, (2019/05/28)
The invention discloses a 2'-C-methyl-substituted nucleoside compound shown in a formula 2 and a pharmaceutically acceptable salt thereof and a preparing method of the 2'-C-methyl-substituted nucleoside compound or the pharmaceutically acceptable salt. The compound has the DOT1L enzyme inhibitor activity, and can be applied to preparing medicines for treating or preventing cancer. The formula is defined in the description.
5'-Deoxidation-5'-isopropyl-substituted-amino nucleoside compound and preparing method and application thereof
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Paragraph 0201-0205, (2019/05/28)
The invention discloses a 5'-deoxidation-5'-isopropyl-substituted-amino nucleoside compound shown in a formula 7, a preparing method of the compound shown in the formula 7 and application of the compound shown in the formula 7 to preparing a 5'-deoxidation-5'-polysubstitution amino nucleoside compound 1 as a midbody. The formula is defined in the description.
N-t-butyloxycarboryl protected heterocyclic compound and preparation method thereof and method for preparing C-nucleoside analogue by N-t-butyloxycarboryl protected heterocyclic compound
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Paragraph 0188-0192, (2019/05/28)
The invention belongs to the field of chemical synthesis and particularly discloses an N-t-butyloxycarboryl protected heterocyclic compound shown in a general formula 5 as shown in the specification,a preparation method of the N-t-butyloxycarboryl protected heterocyclic compound and a method for preparing C-nucleoside analogue by the N-t-butyloxycarboryl protected heterocyclic compound. In the compound 5, Hal is selected from chlorine, bromine and iodine; Z is selected from CR0 or nitrogen; R0 refers to H, halogen, a cyano group, C1-C6 straight chain or branched alkyl, C2-C6 straight chain orbranched alkenyl or C2-C6 straight chain or branched alkynyl. In existing documents, synthesized C-nucleosides are mainly beta-C-nucleosides, but stereoselectivity of beta: alpha is unsatisfactory, and expensive synthesis raw materials are consumed while problems of product separation and purification exist. According to the method, an alpha-C-nucleoside product 8 or a beta-C-nucleoside product 3is controllably synthesized by starting from the easy-to-prepare low-cost compound 5, and high stereoselectivity, high yield, high repeatability and remarkable advantages are realized.