- Application of nicotinamide riboside aromatic formate compound and composition thereof and compound crystal form
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The invention provides application of a nicotinamide riboside triaryl formate compound and a composition thereof in improving the level of coenzyme I (NAD) in the human body, improving health conditions or treating related diseases, and a compound in a crystal form shown in the formula (II-1). The structure of the nicotinamide riboside triaryl formate compound is as shown in a formula (I). As a synthesis precursor of NAD, compared with nicotinamide nucleoside, the nicotinamide nucleoside triaryl formate compound not only can effectively improve the level of NAD in the human body, but also is easier to prepare, the cost is remarkably reduced, and the nicotinamide nucleoside triaryl formate compound has remarkable industrial application advantages.
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- Novel synthesis method of nicotinamide ribose
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The invention discloses a novel synthesis method of nicotinamide ribose. According to the method, 2,3,4,5-tetrabenzoyloxy ribose is added into an alcoholic solution; acetyl chloride is dropwise added;chlorination reaction is performed; a chlorination product and nicotinamide are condensed; benzoyl is removed from a condensation product in sodium methoxide; stirring and purification are performedthrough an organic solvent; and crystallization is performed to obtain a finished product. The novel synthesis method has the advantages that the 2,3,4,5-tetrabenzoyloxy ribose is used as a starting material; ribose 2-benzoyl is selectively chloridized by the acetyl chloride; a product with beta-nicotinamide riboside as a main ingredient is generated; a catalyst is common and easy to obtain; the cost can be effectively reduced; the reaction design ingredients are simple; post treatment is simple; after deprotection, a protective agent and alpha impurities are removed by the organic solvent; and the high-purity finished product can be obtained through recrystallization.
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Paragraph 0022; 0052-0053; 0055-0056; 0058-0059; 0061-0062
(2020/11/22)
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- PROCESS FOR THE PREPARATION OF NICOTINAMIDE RIBOSIDE CHLORIDE DERIVATIVES
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It relates to a process for the preparation of nicotinamide riboside chloride of formula (I) wherein R1-R4 are as defined herein, comprising the following steps: a) reacting a riboside precursor wherein the hydroxyl groups at positions 1, 2, 3 and 5 of the ribose are protected with hydroxyl protective groups; with nicotinamide in the presence of a Lewis acid selected from SnCI4 and TiCI4 in an appropriate solvent, to give the corresponding protected nicotinamide riboside chloride compound, wherein the hydroxyl groups at positions 2, 3 and 5 are protected with hydroxyl protective groups; and b) removing the protective groups of the compound obtained in step a) to give a compound of formula (I). It also relates to a process for the preparation of the protected nicotinamide riboside chloride compound.
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Page/Page column 15-16
(2019/07/13)
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