- Method for synthesizing monoamine-protected piperazine-(R/S)2-formate
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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.
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Paragraph 0032-0034
(2021/02/06)
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