181955-79-3Relevant articles and documents
Method for synthesizing monoamine-protected piperazine-(R/S)2-formate
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Page/Page column 0021-0023, (2021/02/06)
The invention discloses a method for synthesizing monoamine-protected piperazine-(R/S)2-formate, wherein the method comprises the steps: by using 2-piperazinecarboxylate as a raw material, protecting1,4-site amines by using different protective groups, and salifying by using different chiral amines, resolving to obtain a single chiral compound; and finally, using pyridine or DMAP and other pyridine analogues as an alkali, reacting oxalyl chloride, triphosgene, phosgene, thionyl chloride and other similar acyl chlorides in anhydrous tetrahydrofuran, 2-methyl tetrahydrofuran or toluene and other solvents, and finally adding methanol, ethanol, isopropanol, benzyl alcohol and other alcohol reagents to generate the target product capable of removing carboxylic acid ortho-amino protecting groups in a positioned manner and esterifying carboxylic acid. Amino groups on piperazine are separately protected through simple three-step reaction, chiral resolution is performed by utilizing the characteristics of acid, finally, protonated intermediates are formed through organic alkali and carboxylic acid, anhydride is formed by the protonated intermediates and ortho-amino groups, formic acid esterification is performed by utilizing alcohol to replace ring opening, and a final product is obtained.
Piperazine compound and application thereof in preparation of chemokine receptor CCR2 antagonist
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Paragraph 0180-0184, (2020/07/28)
The invention relates to a piperazine compound as shown in a formula (I) and an application of the piperazine compound in preparation of a chemokine receptor CCR2 antagonist or a medicine for treatingCCR2-mediated diseases.
SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Page/Page column 28-29, (2018/03/01)
Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.