- Synthesis method of aztreonam main ring synthesis intermediate N-carbobenzoxy-L-threonine amide
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The invention provides a synthesis method of aztreonam main ring synthesis intermediate N-carbobenzoxy-L-threonine amide, which comprises the following steps: 1) adding an L-threonine solid and methanol into a reaction kettle, stirring, cooling, dropwisely adding thionyl chloride, carrying out heating reflux reaction, and drying a solvent by distillation; (2) adding methanol into a reactant obtained in the step (1) for dissolving, heating and pressurizing, introducing liquid ammonia, keeping the temperature and the pressure, evaporating the liquid ammonia after the reaction is finished, and evaporating the solvent to dryness; and 3) adding water into a reaction product obtained in the step 2) for dissolving, dropwise adding benzyl chloroformate, dropwise adding an acid-binding agent solution to control the pH value of the reaction system to obtain intermediate N-carbobenzoxy-L-threonine amide, and carrying out filter pressing and drying to obtain a solid.
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Paragraph 0018-0024
(2020/05/01)
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- PROCESS AND INTERMEDIATES FOR SYNTHESIS OF PEPTIDE COMPOUNDS
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Disclosed is a new process and intermediates for preparing dipyrrolidine peptide compounds such as, for example, rapastinel. Advantageously, the process may be industrially scalable and cost-effective and use less toxic reagents and/or solvents. Further, the process may be used to prepare peptide compounds having improved purity.
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Paragraph 0171; 0172
(2019/02/13)
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- HEMIAMINAL-TAG FOR PROTEIN LABELING AND PURIFICATION
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The invention pertains to the synthesis, isolation, and characterization of hemiaminal for selective labeling of peptides, proteins, antibodies, and organic fragments with -C(=0) CH2NH2 and derivatives with -CH2NH2 group over -C(=0) CHRNH2 group (where R≠H). The invention also pertains to the method of single-site immobilization of proteins through N-terminus Gly on solid phase. The invention includes late-stage tagging of N-terminus Gly with an affinity tag, 19F NMR probe, and a fluorophore and a method for metal-free protein purification and isolation of analytically pure proteins.
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Page/Page column 22; 24
(2018/06/30)
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- Synthetic method for chiral alpha-aminoamide compounds
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The invention provides a synthetic method for chiral alpha-aminoamide compounds, belongs to the technical field of organic synthetic methodology, and concretely relates to a synthetic method for chiral alpha-aminoamide compounds, wherein the method has a simple process, low costs and good economy. The method comprises the following steps: 1, performing ammonolysis: adding substituted chiral alpha-aminocarboxylate hydrochloride into concentrated ammonia water, performing stirring for 4-12h under a room temperature, wherein each 1mmol substituted chiral alpha-aminocarboxylate hydrochloride is corresponding to 2-8mL the concentrated ammonia water; 2, after a reaction is finished, performing distillation for removing ammonia water after the reaction to obtain crude products chiral alpha-aminoamide compounds; and 3, performing filtration on the obtained crude products chiral alpha-aminoamide compounds by adopting a manner of adding a solvent or performing purification on the obtained crude products chiral alpha-aminoamide compounds through a manner of column chromatography which uses ammonia water as a mobile phase to obtain the products chiral alpha-aminoamide compounds. Compared with the prior art, a large number of an ammonia gas for ammonolysis is not needed in the method, the process and post-treatment are simple, costs are low and reaction time is short.
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Paragraph 0056; 0057; 0058; 0064; 0065
(2018/01/11)
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- PROCESSES FOR SYNTHESIS OF DIPYRROLIDINE PEPTIDE COMPOUNDS
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Disclosed is a new process for preparing dipyrrolidine peptide compounds such as, for example, GLYX-13. Advantageously, the process may be industrially scalable and cost-effective and use less toxic reagents and/or solvents. Further, the process may be used to prepare peptide compounds having improved purity.
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Paragraph 00103-00107
(2017/12/27)
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- Novel method for preparing levetiracetam
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The invention discloses a novel method for preparing levetiracetam. The method employs L-threonine as a raw material and is used to prepare levetiracetam through steps of amidation of carboxyl, acylation of amino, cyclization, sulfonylation, reduction and the like. The provided method for preparing levetiracetam employs the raw material natural amino acid L-threonine, the raw material source is wide and low in price, the reaction demanded conditions and the reaction process are simple, the total yield is relatively high, and the method is suitable for industrialized production.
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Paragraph 0029
(2016/12/12)
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- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Paragraph 00110; page 39
(2014/08/19)
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- Preparation of amino acid amides
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A process for making amino acid amides, comprising reacting an amino acid, or acid salt of an amino acid, with a halogenating agent, or with a substance that reacts with carboxylic acids to form a leaving group, to form an intermediate, then reacting the intermediate with ammonia. When the amino acid or acid salt is enantiomerically pure, the amide will be a stereoisomer. An amide made by the process can be used to form levetiracetam.
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Page/Page column 2
(2008/06/13)
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- Monobactams. Stereospecific Synthesis of (S)-3-Amino-2-oxoazetidine-1-sulfonic Acids
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A facile, stereospecific synthesis of 3-amino-2-oxoazetidine-1-sulfonic acids (monobactams) by the cyclization of acyl sulfamates derived from β-hydroxy amino acids is described.
- Floyd, David M.,Fritz, Alan W.,Cimarusti, Christopher M.
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p. 176 - 178
(2007/10/02)
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