926276-09-7Relevant articles and documents
N-methyl-D-aspartate receptor modulators and methods of making and using same
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Page/Page column 67; 68; 69, (2018/06/25)
Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
Amide derivative, preparation method of amide derivative, and application of amide derivative to pharmacy
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Paragraph 0110; 0126; 0127; 0128; 0129; 0130, (2017/08/30)
The invention provides an amide derivative, a preparation method of the amide derivative, and application of the amide derivative to pharmacy. The amide derivative compound is selected from one of the following structures. The compound can be used for preparing medicines in the fields of local anaesthesia or analgesia. (The formulas are as shown in the description).
Preparation method for bicyclic pyrrolidine intermediate of telaprevir
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Paragraph 0020; 0032, (2017/01/17)
The invention discloses a preparation method for a bicyclic pyrrolidine intermediate of telaprevir. The intermediate is (1S,3alphaR,6alphaS)-octahydrocyclopenta[c]pyrrole-1-carboxylic acid-ethyl ester hydrochloride. The preparation method comprises the following steps: (1) with 3-azabicyclo[3.3.0]octane hydrochloride as a raw material, carrying out Boc2O protection under the action of inorganic base so as to obtain an intermediate 1; (2) dissolving the intermediate 1 in an organic solvent, adding chiral organic ligand, carrying out a reaction with lithium alkyl at -70 DEG C for 2 h under the protection of nitrogen and introducing dry carbon dioxide so as to obtain an intermediate 2; and (3) adding the intermediate 2 into a saturated hydrogen chloride ethanol solution and carrying out a heating reflux reaction for 3 h so as to obtain the target compound. The preparation method provided by the invention has the advantages of short synthesis route, low cost, high product yield and optical purity and easiness in realization of large-scale production.