- Pyridone-containing polycyclic derivative inhibitor as well as preparation method and application thereof
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The invention relates to a pyridone-containing polycyclic derivative inhibitor as well as a preparation method and an application thereof. In particular, the present invention relates to a compound represented by general formula (I), a preparation method
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Paragraph 0163; 0174-0176
(2021/05/12)
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- Efficient Synthesis of a Key Intermediate for Baloxavir Marboxil from a Greener Starting Material: Ethylene Glycol
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In this article, a robust and scalable process to prepare the key intermediate 7-(benzyloxy)-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione (1) for the synthesis of the influenza antiviral drug baloxavir marboxil is described. The process is based on a novel preparation of 2-(2,2-dimethoxyethoxy)ethanamine5employing inexpensive and readily available ethylene glycol as the starting material with more convenient manipulation and fewer environmental hazards compared with the original routes starting with ethanolamine or its derivatives. Large-scale applicability of this new route has been successfully demonstrated on kilogram-scale production to afford 700 grams of1with 99.3% purity in 31% yield over six steps. With such satisfactory quality, baloxavir marboxil is eventually furnished with excellent purity (>99.5%, single impurity 0.1%). Meanwhile, the corresponding impurity profile is studied in detail.
- Wang, Zhongqing,Zhou, Zihong,Kou, Jingping,Wu, Shuming,Xu, Yongbo,Zeng, Jiebin
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p. 2081 - 2089
(2021/09/28)
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- Preparation method of baloxavir intermediate
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The invention relates to the technical field of synthesis of medical intermediates, in particular to a preparation method of a baloxavir intermediate, wherein the baloxavir intermediate is 2,-(2-aminoethoxy)-1, 1-dimethoxyethane. The synthesis route of the baloxavir intermediate specifically comprises the following steps: 1) mixing an alkaline reagent and ethanolamine to obtain a mixed solution, and heating; 2) adding chloroacetaldehyde dimethyl acetal into the mixed solution, stirring, and reacting; and 3) after the reaction is finished, adding ice water and dichloromethane for post-treatment, concentrating an organic phase, and rectifying to obtain the 2,-(2-aminoethoxy)-1, 1-dimethoxyethane. The method is high in product purity, low in cost, simple to operate, mild in condition and suitable for industrial popularization.
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Paragraph 0031-0039
(2021/10/27)
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- Sulfur-containing heterocyclic compound and preparation method thereof
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The invention relates to a sulfur-containing heterocyclic compound and a preparation method thereof. Specifically, the invention discloses a preparation method of a compound A. The preparation methodcomprises the following step: in an organic solvent, und
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Paragraph 0096-0098
(2020/11/09)
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- Purification method of oxoethylamine compound
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The invention provides a purification method of an oxoethylamine compound, belonging to the field of pharmaceutical chemicals. According to the method, an oxoethylamine compound is subjected to salifying, extracting, dissociating and re-extracting to obtain the high-purity oxoethylamine compound. The product produced by the method has the characteristics of high purity, high yield, low cost, simple operation and stable process.
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Paragraph 0045-0061
(2020/09/09)
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- Preparation method of dialkoxy amine compound
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The invention provides a preparation method of a dialkoxy amine compound, and belongs to the field of pharmaceutical chemical industry. The method comprises the following steps: reacting ethylene glycol with an alkali, and treating to obtain a hydroxyl-substituted dialkoxy compound; and adding a protective reagent, an amine source compound and hydrogen, and carrying out protection, amine source replacement, reduction and other steps to obtain the final product. According to the method provided by the invention, the required dialkoxy amine compound can be effectively prepared, and good conditions are provided for further preparing a target compound; and the method has the advantages of high product purity, high yield, simple operation and the like.
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- STEREOSELECTIVE PROCESS FOR PREPARING SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVES
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The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity. In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof.
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Paragraph 0508; 0512
(2020/08/20)
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- Substituted polycyclic pyridone compound and prodrug thereof
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The invention provides a deuterium-substituted polycyclic pyridone compound, a prodrug thereof, a composition containing the compound and application of the composition. The deuterium-substituted polycyclic pyridone compound is the compound shown in the formula (I) or a tautomer, stereoisomer, prodrug, crystalline form, pharmaceutically acceptable salt, hydrate or solvent compound thereof. The compound and the composition show the cap-dependent endonuclease inhibitory activity and have superior pharmacokinetic properties.
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Paragraph 0173-0176; 0179; 0180
(2019/10/23)
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- Substituted polycyclic pyridone derivative and its crystal
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Substituted polycyclic pyridone derivative of the manufacturing method. Formula (I): (In the formula, R1 Is hydrogen, unsubstituted alkyl or other protecting group. ) Shown in compound, and/or magnesium salt in the presence of a sodium salt, Formula: R2 - OH (In the formula, R2 A non-substituted alkyl. ) Is reacted with a compound represented by the, formula (II): (In the formula, R2 The same significance as described above. ) Production of a compound represented.
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Paragraph 0043
(2018/06/30)
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