1985605-59-1Relevant articles and documents
SOLID STATE FORMS OF BALOXAVIR MARBOXIL
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Paragraph 00141, (2020/09/19)
The present disclosure relates to solid state forms of baloxavir marboxil, processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
A MEDICAMENT FOR TREATING INFLUENZA CHARACTERIZED BY COMBINING A CAP-DEPENDENT ENDONUCLEASE INHIBITOR AND AN ANTI-INFLUENZA DRUG
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, (2020/08/30)
A medicament characterized in that (A) a compound represented by the formula (I): its pharmaceutically acceptable salt, or a solvate thereof, wherein P is hydrogen or a group to form a prodrug; A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is each independently CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A4 is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A are each independently hydrogen, halogen, alkyl, or the like; R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together with an adjacent carbon atom to form non-aromatic carbocycle or non-aromatic heterocycle; n is any integer of 1 to 2; and R1 is or the like, is combined with (B) compound(s) having an anti-influenza activity, its pharmaceutically acceptable salt or a solvate thereof and/or an antibody having anti-influenza activity, is useful for treating or preventing influenza.
Method for synthesizing novel anti-influenza drug
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, (2020/10/04)
The invention discloses a method for synthesizing a novel anti-influenza drug baloxavir marboxil. The method comprises the following steps: directly docking a thiosalicylic acid compound 1 and a 1-(halogenated methyl)-2,3-difluorobenzene compound 2 serving as initial raw materials so as to obtain a compound 3; performing PPA ring closure to obtain a 7,8-difluorodibenzo[b,e]thiozepine-11(6H)-one compound 4, and obtaining a key chiral thiazem intermediate compound 5 under catalysis of a chiral enzyme; directly condensating the compound 5 and a key chiral fragment compound 6 by virtue of a Mitsubobu reaction so as to obtain a compound 7; finally performing dealkylation protection, and condensating with ((methoxycarbonyl)oxo)4-methyl-toluenesulfonate, so as to obtain the final product compound9, namely the baloxavir marboxil. According to the synthetic route, the process operation magnification difficulty of the route is reduced, the production of by-products is reduced, the product purity is improved, and the cost of the route is reduced.
