- Synthesis method of 3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid
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The invention discloses a synthesis method of 3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid. The synthesis method sequentially comprises the following steps: S1, condensing 4-chloroacetoacetate and benzyl alcohol to obtain an intermediate I; S2, condensing the intermediate I with N,N-dimethylformamide dimethyl acetal to obtain an intermediate II; S3, performing ring closing on the intermediate IIand oxalic acid diester to obtain an intermediate III; and S4, decarboxylating the intermediate III in an acidic aqueous solution to obtain a target product. The method has the advantages of simple steps, mild conditions, cheap and easily available raw materials, and reduction of the cost of a target patent medicine.
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Paragraph 0043; 0080-0086
(2021/03/31)
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- Practical Synthetic Method for the Preparation of Pyrone Diesters: An Efficient Synthetic Route for the Synthesis of Dolutegravir Sodium
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A highly efficient and practical synthetic method for the preparation of pyrone diesters was established. The pyrone diester 3c can be prepared from readily available starting materials on a multihundred gram scale. The pyrone diester 3c can easily be converted to dolutegravir sodium (1). The synthetic route demonstrated herein provides an efficient and atom-economical synthetic method for preparing this potent anti-HIV agent.
- Yasukata, Tatsuro,Masui, Moriyasu,Ikarashi, Fumiya,Okamoto, Kazuya,Kurita, Takanori,Nagai, Masahiko,Sugata, Yoshihide,Miyake, Naoki,Hara, Shinichiro,Adachi, You,Sumino, Yukihito
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p. 565 - 570
(2019/03/26)
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- Synthesis method of dolutegravir intermediate, and related substance detection method thereof
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The invention discloses a synthesis method of a dolutegravir intermediate, and a related substance detection method thereof. 4-chloroacetoacetic acid methyl ester and phenylcarbinol are adopted as starting materials, and the dolutegravir intermediate i is obtained through four steps of reaction; the reaction conditions are simple, only methylbenzene is used as a solvent in reaction, the raw materials are easy to get, the obtained product is treated and purified through column chromatography, the yield of the product obtained by each step reaches up to 90 percent or above, and the synthesis method is suitable for industrial production; the related substance detection method of the dolutegravir intermediate i adopts high performance liquid chromatography; through testing, the content of thedolutegravir intermediate i related substance is 99.6 percent, the separation degree of each impurity is larger than 3.0, and the separation degree is better.
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Paragraph 0038; 0039; 0040; 0041
(2018/06/26)
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- PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY
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A process for preparing a compound represented by formula (Y1) or (Y2) [wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R1d is hydrogen, halogen, or the like; R2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R4d is a lower alkyl optionally substituted with substituent E, or the like; and R6d is a lower alkyl group optionally substituted with substituent group E, or the like].
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Paragraph 0124
(2013/06/27)
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- METHOD OF PRODUCING PYRONE AND PYRIDONE DERIVATIVES
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The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
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Page/Page column 24-25
(2012/02/03)
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