Preparation methods of niraparib and intermediate of niraparib as well as intermediate compound
The invention discloses a preparation method of an intermediate of niraparib. The intermediate is as shown in the following formula. The preparation method comprises the following steps of using (S)-oxazolidone and p-bromophenylacetic acid as initial raw materials, and carrying out amide condensatio...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention discloses a preparation method of an intermediate of niraparib. The intermediate is as shown in the following formula. The preparation method comprises the following steps of using (S)-oxazolidone and p-bromophenylacetic acid as initial raw materials, and carrying out amide condensation, Michael addition, the reduction of ester and amide, the synthesis of sulfonyl ester, ammonification ring formation and a reaction of salt formation with an organic acid, so as to obtain the intermediate. The invention also discloses a preparation method of the niraparib and an intermediate compound of the niraparib. The preparation methods provided by the invention are low in cost and are suitable for industrialized production; raw materials are easily obtained and the yield is higher. The formula structure is shown in the description.
本发明公开了种尼拉帕尼的中间体的制备方法,如下式所示,其包含下列步骤:以(S)-恶唑烷酮与对溴苯乙酸为起始原料,进行酰胺缩合,迈克尔加成,脂和酰胺的还原,磺酰脂的合成,氨化成环,与有机酸成盐的反应,即可。本发明还公开了尼拉帕尼的制备方法及其中间体化合物。本发明的制备方法成本低,原料易得,产率较高,适于工业化生产。 |
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