1985607-83-7Relevant articles and documents
Pyridazone derivative and its uses
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Paragraph 0163, (2022/01/12)
The present invention belongs to the pharmaceutical field, specifically relates to a pyridazone derivative and its uses, compounds thereof and pharmaceutically acceptable salts, solvates including hydrates, polycrystallines, prodrugs, co-crystallines, tau
Synthesis method of baloxavir marboxil intermediate
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Paragraph 0029-0033, (2021/05/19)
The invention discloses a synthesis method of a baloxavir marboxil intermediate. The synthesis method comprises the following steps of: taking 7,8-difluorodibenzo[B,E]thiophene-11(6H)-ketone as a raw material, adopting chloro(R,R)-N-(tosyl)-1,2-diphenyl ethylene diamine(chloro)(p-propyl toluene) ruthenium (II) or chloro(S,S)-N-(tosyl)-1,2-diphenyl ethylene diamine(chloro)(p-propyl toluene) ruthenium (II) as a catalyst, reducing carbonyl into chiral alcohol so as to obtain an intermediate namely chiral 7,8-difluoro-dihydrodibenzo[b,e]thiepin-11-ol for synthesizing baloxavir marboxil. The optical purity of baloxavir marboxil synthesized from the intermediate is 98.0% or more, the subsequent purification processes are reduced, the yield is increased, the cost is reduced, and the synthesis method is more suitable for commercial production.
Dibenzo seven-membered ring derivative as well as preparation method and application thereof
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, (2021/03/31)
The invention relates to a dibenzo seven-membered ring derivative as well as a preparation method and application thereof. The chemical structure of the dibenzo seven-membered ring derivative is shownas a formula (I), and X1 and X2 are respectively and independently selected from H, F, Cl, Br or I. The preparation method has easily available raw materials, and can ensure continuous supply and production; the raw materials are cheap and have the cost advantage; and thiophenol or sodium thiophenol is not used, so that the method is more environment-friendly and is also beneficial to the body health of related personnel. 7,8-difluorodibenzo[b,e]thiazepine-11(6H)-one as one of the products can further react to obtain 7,8-difluoro-6,11-dihydrobenzo[c][1]benzothiepin-11-ol, and the 7,8-difluoro-6,11-dihydrobenzo[c][1]benzothiepin-11-ol can be used as an important intermediate for preparing a drug baloxavir, so that baloxavir preparation cost is reduced.
Preparation method of sulfur-containing hetero-seven-membered ring compound
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, (2021/06/13)
The invention relates to a preparation method of a sulfur-containing hetero-seven-membered ring compound. The method comprises the following steps: carrying out halogenation reaction, nucleophilic substitution, acylation, cyclization, reduction and the li
Pyridone-containing polycyclic derivative inhibitor as well as preparation method and application thereof
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Paragraph 0163; 0210-0213, (2021/05/12)
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
Preparation method of baloxavir key intermediate and intermediate thereof
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Paragraph 0039; 0044-0046; 0051-0053; 0056-0057; 0060, (2020/11/02)
The invention discloses a preparation method of a baloxavir key intermediate and the intermediate thereof. The method includes subjecting 3,4-difluoro-2-methyl benzaldehyde shown as a formula (I) as araw material to a bromination reaction to obtain 3,4-di
Xofluza sulfur-containing heterocyclic compound, intermediate and preparation method thereof
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, (2020/03/17)
The invention discloses an Xofluza sulfur-containing heterocyclic compound, an intermediate and a preparation method thereof, and provides a preparation method of a compound represented by a formula 5. The preparation method is mild in reaction condition,
Synthesis method of baloxavir marboxil intermediate
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, (2019/08/30)
The invention provides a synthesis method of a baloxavir marboxil intermediate. The invention provides a synthesis method of a compound (III), which is prepared through three steps. The yield is improved, and the production is easy to control. At the same
Development of a Quality Controllable and Scalable Process for the Preparation of 7,8-Difluoro-6,11-dihydrodibenzo[ b, e]thiepin-11-ol: A Key Intermediate for Baloxavir Marboxil
Zhou, Zihong,Wang, Zhongqing,Kou, Jingping,Wu, Shuming,Zhang, Junrong,Yuan, Xi,Wu, Xiwei,Li, Chuan-Hua,Liao, Gaohong
, p. 2716 - 2723 (2019/12/24)
A novel six-step synthesis of 7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-ol (1) is described. Starting with 3,4-difloro-2-methylbenzoic acid and using diphenyl disulfide as an ideal sulfur source effectively solve the problems such as harsh reaction conditions, usage of smelly thiophenol, which might restrict the known process from pilot plant application. Large-scale applicability of this new route has been successfully demonstrated on kilogram-scale production to afford 1 with 98.04% purity in 75% overall yield. Meanwhile, the corresponding impurity profile was thus studied in detail and well documented.
Preparation method of chiral dibenzo[b,e]thiepin-11-ol
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Paragraph 0052-0079; 0084-0089, (2019/08/30)
The invention discloses a preparation method of chiral dibenzo[b,e]thiepin-11-ol. The method comprises the following steps: dissolving a compound 3 into an organic solvent, performing reduction on thecompound 3 under catalysis of (S)-2-R-CBS-oxazaborolidine or (R)-2-R-CBS-oxazaborolidine under the action of borane to obtain the (R)-1 or (S)-1 with high chiral purity. The method provided bythe invention is simple and convenient to operate and suitable for industrial production.
