1985607-70-2

Usage

Uses

Due to the lack of detailed information, the specific applications of (R)-7-(benzyloxy)-6,8-dioxo-1,3,4,6,8,12a-hexahydro-12H-[1,4]oxaazino[3,4-c]pyridino[2,1-f][1,2,4]triazine are not clearly defined. However, given its classification as a heterocyclic compound, it is reasonable to infer that it may have potential uses in various sectors such as:
Used in Pharmaceutical Industry:
(R)-7-(benzyloxy)-6,8-dioxo-1,3,4,6,8,12a-hexahydro-12H-[1,4]oxaazino[3,4-c]pyridino[2,1-f][1,2,4]triazine could be used as an active pharmaceutical ingredient or a key intermediate in the synthesis of drugs, given the importance of heterocyclic compounds in drug development.
Used in Agrochemical Industry:
(R)-7-(benzyloxy)-6,8-dioxo-1,3,4,6,8,12a-hexahydro-12H-[1,4]oxaazino[3,4-c]pyridino[2,1-f][1,2,4]triazine might also serve as a component in the formulation of agrochemicals, such as pesticides or herbicides, where heterocyclic compounds are commonly employed for their bioactivity.
Used in Veterinary Medicine:
(R)-7-(benzyloxy)-6,8-dioxo-1,3,4,6,8,12a-hexahydro-12H-[1,4]oxaazino[3,4-c]pyridino[2,1-f][1,2,4]triazine could potentially be utilized in the development of veterinary drugs or treatments, considering the prevalence of heterocyclic compounds in this field.

Upstream product

• 2136287-59-5 methyl 1-((tert-butoxycarbonyl)amino)-3-(benzyloxy)-4-oxo-1,4-dihydropyridine-2-carboxylic acid 
• 110-91-8 morpholine 
• 119736-16-2 3-(benzyloxy)-1-((tert-butoxycarbonyl)amino)-4-oxo-1,4-dihydropyridine-2-carboxylic acid ethyl ester 
• 1985607-70-2 7-(benzyloxy)-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido [2,1-f][1,2,4]triazine-6,8-diketone 

Downstream Products

• 1985605-59-1 (R)-12-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-7-hydroxy-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione 

Relevant academic research and scientific papers

Preparation method of fused ring pyridone compound

The invention relates to a preparation method of a fused ring pyridone compound, and belongs to the field of medicinal chemistry. The preparation method comprises the following steps: reacting a raw material with diglycolamine to obtain an intermediate compound, or oxidizing and cyclizing the intermediate compound to obtain a fused ring pyridone compound. According to the method, cheap and easily available diglycolamine is used, so that the reaction steps can be reduced, the operation is simplified, the material cost is reduced, and industrial large-scale production is facilitated.

Preparation method of balosavir intermediate

The invention relates to a preparation method of a baloxavir intermediate, in particular to a method for efficiently synthesizing the baloxavir intermediate by taking 3-(benzyloxy)-4-oxo-4H-pyran- 2-carboxylic acid as a raw material through three steps of condensation reaction, hydrazinolysis reaction and cyclization reaction. The preparation method of the balosavir intermediate provided by the invention is a preparation method which is high in yield, low in cost, less in three wastes, high in product purity and suitable for industrialization.

Pyridone-containing polycyclic derivative inhibitor as well as preparation method and application thereof

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

Efficient Synthesis of a Key Intermediate for Baloxavir Marboxil from a Greener Starting Material: Ethylene Glycol

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.

Synthesis method of baloxavir marboxil intermediate polycyclic carbamoyl pyridone

The invention provides a synthesis method of a baloxavir marboxil intermediate polycyclic carbamoyl pyridone, which is characterized in that 1-amino-3-(benzyloxy)-N-(2-ethoxyl)-4-oxo-1, 4-dihydropyridine-2-carboxamide and chloroacetaldehyde are subjected to ring closing under the action of alkali, and the baloxavir marboxil intermediate polycyclic carbamoyl pyridone is obtained in one step. Compared with the prior art, 1-amino-3-(benzyloxy)-N-(2-ethoxyl)-4-oxo-1, 4-dihydropyridine-2-carboxamide and chloroacetaldehyde are subjected to ring closing under the action of alkali to obtain the polycyclic carbamoyl pyridone, traditional multi-step synthesis is improved into a one-pot method, reaction operation is obviously simplified, and the method has the advantages of high production efficiency, low cost, small pollution and suitability for industrial production.

A series of new polycyclic carbamoyl pyridone analogues were synthesized by using chloroacetaldehyde as a substrate

A facile, universal and economical method was developed for the synthesis of polycyclic carbamyl pyridone analogues of Baloxavir marboxil from the cyclization of chloroacetaldehyde with o-aminoamide derivatives. In this method, without any other catalysts or additives, the polycyclic carbamoyl pyridone analogues can be obtained by ring closure of o-aminoamide derivatives and chloroacetaldehyde under the action of a base, and no harsh reaction conditions are required. The method operation is simple and suitable for industrial production. A series of polycyclic carbamyl pyridone analogues were prepared in moderate to excellent yields.

Preparation method of balosavir intermediate

The invention discloses a preparation method of a balosavir intermediate, which comprises the following steps (R1 is selected from C1C4 alkyl;): (1) carrying out substitution reaction on a compound 20 or a compound 27 and aminoethanol under an alkaline co

Preparation method of balosavir intermediate

The invention discloses a preparation method of a baloxavir intermediate (R)-7-(benzyloxy)-3, 4, 12, 12a-tetrahydro-1H-[1, 4]oxazine[3, 4-c]pyrido[2, 1-f][1, 2, 4]-triazine-6, 8-diketone, and belongsto the field of drugs. According to the method, 3-benzyloxy-1-Boc amino-4-carbonyl-1, 4-dihydropyridine-2-carboxylic acid methyl ester and a chiral substrate L-serine ester are taken as raw materialsto carry out condensation reaction, substitution reaction and cyclization decarboxylation reaction to synthesize a baloxavir key intermediate (R)-7-(benzyloxy)-3, 4, 12, 12a-tetrahydro-1H-[1, 4]oxazine[3, 4-c]pyrido[2, 1-f][1, 2, 4]-triazine-6, 8-diketone and creatively develop the synthetic route for synthesizing the baloxavir intermediate (R)-7-(benzyloxy)-3, 4, 12, 12a-tetrahydro-1H-[1, 4]oxazine[3, 4-c]pyrido[2, 1-f][1, 2, 4]-triazine-6, 8-diketone. Compared to the traditional route, the preparation method has the advantages of the high yield, low cost, no need of resolution, the high chiral purity, convenience in industrialization and the like.

Preparation method of baloxavir intermediate

The invention relates to a preparation method of a baloxavir intermediate (compound VI). The preparation method comprises the following steps: taking 3-morpholinone and 3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid as initial raw materials; carrying out amino protection on 3-morpholinone to obtain a compound I, and carrying out selective reductive amination on the compound I and ammonium formatein the presence of a catalyst and a chiral ligand to obtain a chiral compound II; reacting the 3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid with hydroxylamine hydrochloride to obtain a compound III,and carrying out an esterification reaction on the compound III and alcohol to obtain a compound IV; and carrying out an SN2 reaction on the compound IV and a chiral compound II to obtain a compoundV, removing a protecting group from the compound V under the action of a catalyst, and carrying out cyclization to obtain the compound VI. The method provides a simple and convenient industrial production route for the baloxavir intermediate, and has the advantages of simple reaction operation, avoidance of chiral resolution, few steps and low cost.

Condensed ring pyridone derivative as well as preparation method and application thereof

The invention discloses a condensed ring pyridone derivative as well as a preparation method and an application thereof. The condensed ring pyridone derivative is a compound shown in a formula I, or an optical isomer, an enantiomer, a diastereomer, a raceme or a racemic mixture thereof, or a solvate, a prodrug or pharmaceutically acceptable salt thereof. The invention also discloses the application of the compound and a pharmaceutical composition containing the compound in preparation of drugs for preventing and/or treating viral infection diseases. The viral infectious disease is a disease caused by a virus having a cap-dependent endonuclease, and more specifically, an infectious disease caused by influenza A or influenza B.