946859-86-5Relevant academic research and scientific papers
Synthetic method of florfenicol intermediate
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Paragraph 0151-0156, (2019/07/04)
The invention relates to a synthetic method of a florfenicol intermediate. The synthetic method comprises following specific steps: compound II is dissolved in an organic solvent, under alkaline conditions, methyl sulfonyylation is carried out so as to obtain compound III; the compound III is subjected to ring closing reaction under alkaline conditions so as to obtain compound IV; and the compoundIV is subjected to fluorination ring opening reaction so as to obtain the florfenicol intermediate I. The synthetic method is novel in design, mild in conditions, and convenient in operation, and issuitable for industrialized production.
Florfenicol intermediate synthesis method
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Paragraph 0177-0181, (2019/07/04)
The invention belongs to the field of synthesis of pharmaceutical raw materials, and specifically discloses a florfenicol intermediate synthesis method, which comprises: (1) carrying out a reaction ona compound (II) and an acylating reagent in an organic solvent to form a compound (III); (2) carrying out a reaction on the compound (III) and an oxidizing agent in an organic solvent in the presenceof a catalyst to form a compound (IV); (3) carrying out a reaction on the compound (IV) and a fluorinating reagent in an organic solvent to form a compound (V); and (4) carrying out acidolysis on thecompound (V) in an organic solvent, and carrying out deprotection to obtain a compound (I), wherein various groups in the formulas are defined in the specification. According to the present invention, the florfenicol intermediate can be used for preparing florfenicol; and the method has characteristics of novel design, mild conditions and simple operation, and is suitable for industrial production.
A (1R, 2R) - 1 - substituted phenyl - 2 - amino - 1, 3 - propanediol
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, (2017/08/24)
The invention belongs to the technical field of pharmaceutical chemistry, and particularly relates to a synthesis method of (1R,2R)-1-substituted-phenyl-2-amino-1,3-propanediol. The preparation method comprises the following steps: rearranging 2-(N-substituted-oxyformacyl-substituted-benzoylamino)acetate to obtain 2-substituted-oxyformamido-3-substituted-phenyl-3-oxopropionate; and carrying out asymmetric transfer hydrogenation with dynamic resolution to obtain (2S,3S)-alpha-substituted-amino-beta-hydroxy ester, and carrying out configuration reversion and deprotection to obtain the (1R,2R)-1-substituted-phenyl-2-amino-1,3-propanediol. The method has the advantages of mild conditions and high optical purity, and is simple to operate and suitable for industrial production.
Catalytic asymmetric transfer hydrogenation/dynamic kinetic resolution: an efficient synthesis of florfenicol
Wang, Xinlong,Xu, Lingjun,Yan, Lingjie,Wang, Haifeng,Han, Sheng,Wu, Yan,Chen, Fener
, p. 1787 - 1793 (2018/03/29)
A robust and practical method has been developed for the synthesis of florfenicol (1) starting from commercial available 4-(methylsulfonyl) benzoic acid. The key step in this synthesis was the Ru-chloramphenicol base catalyzed asymmetric transfer hydrogenation of N-Boc α-amino-β-ketoester 5 through a dynamic kinetic resolution, which afforded the key chiral building block, anti-(2S,3S)-α-Boc-amino-β-hydroxyl ester 4, with high diastereoselectivity (92% de) and enantioselectivity (78% ee). The synthesis of a series of novel chloramphenicol base ligands L1–L10 is also included. This protocol could also be used for the asymmetric synthesis of fully synthetic analogs of florfenicol.
Fenicol compounds and methods synthesizing 2-trifluoroacetamido-3-substituted propiophenone compounds
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Page/Page column 17, (2008/06/13)
Methods of preparing compounds of formula (I): wherein Y, Y1, and R2 are defined herein; methods of making D-(threo)-1-aryl-2-acylamido-1-propanol compounds, D-(threo)-1-aryl-2-acylamido-3-fluoro-1-propanol compounds, and D-(threo)-1
