1119-33-1Relevant articles and documents
The Synthesis of the High-Potency Sweetener, NC-00637. Part 3: The Glutamyl Moiety and Coupling Reactions
Ager, David J.,Babler, Scott,Erickson, Robert A.,Froen, Diane E.,Kittleson, Jeannine,Pantaleone, David P.,Prakash, Indra,Zhi, Ben
, p. 72 - 85 (2004)
The synthesis of the high-potency sweetener, NC-00637 (1), required selective preparation of the γ-protected glutamic acid. Coupling of the three components could be performed in any order, but the final route involved N-acylation of the protected L-glutamic acid with the acid chloride derived from (S)-2-methylhexanoic acid. Activation of the α-carboxyl group allowed condensation with 5-amino-2-cyanopyridine (4). Saponification of the γ-ester 19 then provided the sweetener 1.
Synthesis method of vildagliptin
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Paragraph 0031-0033; 0038-0040; 0045-0047, (2020/09/12)
The invention discloses a synthesis method of vildagliptin. The method comprises the following steps: performing esterification reaction on L-glutamic acid and ethanol to obtain L-glutamic acid-gamma-ethyl ester; reducing the L-glutamic acid-gamma-ethyl ester under the action of potassium borohydride to obtain L-proline; mixing L-proline with ethyl chloroformate for reaction to obtain acid anhydride; further reacting the acid anhydride with amine to obtain amide; dehydrating the amide under the action of phosphorus pentoxide to obtain an intermediate 1; performing substitution reaction on theintermediate 1 and chloroacetyl chloride to obtain an intermediate 2; and further reacting the intermediate 2 with 3-amino-1-adamantanol to obtain vildagliptin. The method has the advantages that fewimpurities are generated in the vildagliptin preparation process, the yield of the prepared vildagliptin is high, and compared with the prior art, the process is simpler, and the vildagliptin preparation cost is greatly reduced.
Butyryl glutamic acid derivative as well as composition and application thereof
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Paragraph 0154; 0155, (2018/07/30)
The invention discloses a butyryl glutamic acid derivative as well as a composition and application thereof. The butyryl glutamic acid derivative disclosed by the invention or a racemic modification,stereisomer, geometric isomer, tautomer and solvate or feed-acceptable salt thereof can be applied in the preparation of novel feed additives and feeds. The invention further discloses a feed composition of the butyryl glutamic acid derivative or the racemic modification, the stereisomer, the geometric isomer, the tautomer and the solvate or the feed-acceptable salt thereof. When applied in animalhusbandry, the butyryl glutamic acid derivative provided by the invention has the effect of improving the production performance of animals, such as increasing animal weight increasing rate, decreasing feed conversion ratio and controlling diarrhea rate, and can be applied as an effective, safe novel feed additive.
