134307-32-7Relevant academic research and scientific papers
Benzylation of aldonolactones with benzyl trichloroacetimidate
Jensen, Hanne Stampe,Limberg, Gerrit,Pedersen, Christian
, p. 109 - 112 (1997)
A number of aldono-1,4-lactones have been converted to their perbenzylated derivatives by treatment with benzyl trichloroacetimidate. 2,3,6-Trideoxy-D-erythro-hexono-1,4-lactone could be benzylated in dichloromethane, but lactones containing two or more h
Weinreb Amide Approach to the Practical Synthesis of a Key Remdesivir Intermediate
Xie, Yuanchao,Hu, Tianwen,Zhang, Yan,Wei, Daibao,Zheng, Wei,Zhu, Fuqiang,Tian, Guanghui,Aisa, Haji A.,Shen, Jingshan
, p. 5065 - 5072 (2021)
Currently, remdesivir is the first and only FDA-approved antiviral drug for COVID-19 treatment. Adequate supplies of remdesivir are highly warranted to cope with this global public health crisis. Herein, we report a Weinreb amide approach for preparing the key intermediate of remdesivir in the glycosylation step where overaddition side reactions are eliminated. Starting from 2,3,5-tri-O-benzyl-d-ribonolactone, the preferred route consisting of three sequential steps (Weinreb amidation, O-TMS protection, and Grignard addition) enables a high-yield (65%) synthesis of this intermediate at a kilogram scale. In particular, the undesirable PhMgCl used in previous methods was successfully replaced by MeMgBr. This approach proved to be suitable for the scalable production of the key remdesivir intermediate.
Synthesis and Biological Evaluation of Pyrrolo[2,1-f][1,2,4]triazine C-Nucleosides with a Ribose, 2′-Deoxyribose, and 2′,3′-Dideoxyribose Sugar Moiety
Li, Qingfeng,Lescrinier, Eveline,Groaz, Elisabetta,Persoons, Leentje,Daelemans, Dirk,Herdewijn, Piet,De Jonghe, Steven
, p. 97 - 104 (2018)
The synthesis of hitherto unknown pyrrolo[2,1-f][1,2,4]triazine C-nucleosides is described. Structural variations (chlorine, bromine, iodine, and cyano groups) were introduced at position 7 of 4-aza-7,9-dideazaadenine. In addition, pyrrolo[2,1-f][1,2,4]triazine C-nucleosides bearing a 2′-deoxy-, 2′,3′-dideoxy-, and 2′,3′-dehydrodideoxyribose moiety were also prepared. Among these analogues, the pyrrolo[2,1-f][1,2,4]triazine C-ribonucleosides with either a hydrogen atom or cyano group at position 7 of the nucleobase displayed potent cytotoxic activity in a panel of various cancer cell lines.
Synthesis and evaluation of a collection of purine-like C-nucleosides as antikinetoplastid agents
Bouton, Jakob,Maes, Louis,Karalic, Izet,Caljon, Guy,Van Calenbergh, Serge
supporting information, (2021/01/06)
The kinetoplastid parasites Trypanosoma brucei, Trypanosoma cruzi and Leishmania spp. are the causative agents of neglected tropical diseases with a serious burden in several parts of the world. These parasites are incapable of synthesizing purines de nov
Compound for treating viral infection and preparation method and application of compound
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Paragraph 0149-0154, (2021/08/07)
The invention provides a preparation for treating viral infection and pneumovirus subfamily viral infection, a method, a compound as shown in a formula (I) and a method and intermediate for synthesis of the compound as shown in the formula (I).
Compound containing guanidyl group, and preparation method and application thereof
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Paragraph 0138-0143, (2021/08/07)
The invention provides a preparation containing a guanidino compound and used for treating pneumoviridae virus infection, a method, a compound of a formula I, and a method and an intermediate for synthesizing the compound of the formula I.
Novel compound and application thereof
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Paragraph 0081-0083, (2021/09/08)
The invention relates to a novel compound and application thereof, and also relates to an application of the compound in preparation of antiviral drugs and the like. In particular, AIDS virus is present. Application of hepatitis B virus, paramyxovirus and
ISOMORPHS OF REMDESIVIR AND METHODS FOR SYNTHESIS OF SAME
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Paragraph 0083, (2021/06/04)
A new isoform of 2-ethylbutyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3/4-dihydroxyoxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate (Remdesivir) having increased water solubility is disclosed, along with methods
Method for preparing 2, 3, 5 -tribenzyloxy - D D-ribose -1, 4 - lactone in continuous flow microchannel reactor (by machine translation)
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Paragraph 0040-0081, (2020/09/02)
The method disclosed by the invention has the advantages of simple operation, safety, 3 short 5 - reaction time,1 high 4 - product conversion rate, high product purity and the like 2, 3 and 5 - has the advantages of simple operation, 2 safety 3, 5 - short
Preparation method of 2, 3, 5-tribenzyloxy-D-ribose-1, 4-lactone
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Paragraph 0030-0064, (2020/07/02)
The invention provides a preparation method of 2, 3, 5-tribenzyloxy-D-ribose-1, 4-lactone. In the preparation method, in the oxidation step, sodium bromide/TEMPO is creatively used as a catalyst, sodium hypochlorite serves as an oxidizing agent, a large a
