- SUBSTITUTED BORIC ACID COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND APPLICATION THEREOF
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A substituted boric acid compound, a pharmaceutical composition comprising same, and an application thereof. The substituted boric acid compound is a compound represented by formula (I), or a crystal form, a pharmaceutically acceptable salt, a prodrug, a stereoisomer, a hydrate, or a solvent compound thereof. The boric acid compound has proteasome inhibitory activity, good pharmacodynamic/pharmacokinetic performance, good applicability, and high safety, and can be used for preparing drugs for treating diseases related to proteasomes.
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Paragraph 0038; 0039
(2019/05/10)
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- Synthesis methods of deuterine, hippuric acid-L-menthol ester (2,2-D2) and intermediates thereof
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The invention discloses synthesis methods of deuterine, hippuric acid-L-menthol ester (2,2-D2) and intermediates thereof, wherein the synthesis method includes the steps: (1) carrying out a reaction of glycine with a deuterium aqueous solution of alkali metal deuterium oxide under the action of pyridoxal or salts thereof, to obtain a deuterated reaction solution; and (2) recycling a part of deuterium water from the deuterated reaction solution obtained in the step (1) through reduced pressure distillation, then adding water and benzoyl chloride, carrying out an amidation reaction, and after the end of the reaction, posttreating to obtain hippuric acid (2,2-D2). The raw materials and reagents used in the synthesis method are cheap and easy to obtain, and the operation is simple; the purityand the deuterium abundance of the obtained deuterated reagents are high.
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Paragraph 0047; 0054-0055; 0058
(2018/10/26)
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- Development and Scale-Up of Stereoretentive α-Deuteration of Amines
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A stereoretentive deuteration of amino acids and amines has been developed using ruthenium on carbon catalyst, hydrogen gas at atmospheric pressure, and deuterium oxide as a source of deuterium. The process was successfully scaled-up, avoiding the use of expensive and sensitive catalyst and avoiding the use of deuterium gas under pressure. High deuterium incorporation and high yield of labeled compounds were obtained by a simple filtration process.
- Michelotti, Alessia,Rodrigues, Fabien,Roche, Maxime
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supporting information
p. 1741 - 1744
(2017/11/24)
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- Measurement of biosynthesis and breakdown rates of biological molecules that are inaccessible or not easily accessible to direct sampling, non-invasively, by label incorporation into metabolic derivatives and catabolitic products
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Methods of determining rate of biosynthesis or breakdown of biological molecules from metabolic derivatives and catabolic products are disclosed herein. In particular, methods of measuring the rates of biosynthesis and breakdown of biological molecules inaccessible or not easily accessible to direct sampling by sampling metabolic derivatives and catabolic products in accessible biological samples are disclosed herein.
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- Simple and efficient preparation of (R)- and (S)-enantiomers of α-carbon deuterium-labelled α-amino acids
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A procedure for the synthesis of (R)- and (S)-enantiomers of α-carbon deuterium-labelled α-amino acids, exemplified for (R)- and (S)-[2-2H1]-Leu is described. Starting from the respective (S)- or (R)-enantiomer or from the racemic mixture of an α-amino acid the selective proton exchange at the α-carbon is carried out by racemization via a Schiff base in monodeuterated acetic acid as solvent which serves as deuterium source. After N-protection the racemic mixture is liquid chromatographically separated into the individual (R)- and (S)-enantiomers on preparative scale employing a chiral anion exchanger based on carbamoylated quinine as chiral selector. After deprotection the enantiomerically pure products can be obtained in good yields.
- Mitulovi, Goran,Laemmerhofer, Michael,Maier,Lindner, Wolfgang
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p. 449 - 461
(2007/10/03)
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