Preparation method of 7H-pyrrolo [2, 3-d] pyrimidine derivative and synthetic intermediate of 7H-pyrrolo [2, 3-d] pyrimidine derivative

The invention relates to a preparation method of a 7H-pyrrolo [2, 3-d] pyrimidine derivative and a synthetic intermediate thereof. The present invention provides processes for the preparation of 7H-pyrrolo [2, 3-d] pyrimidine derivatives useful as inhibitors of Janus Kinases (JAK), intermediates the...

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Hauptverfasser: BORHOLD JUERGEN, TAKIGUCHI HIROMU, VYSOE PER, JENSEN KIRK L, HIGASHI AKINOBU, INABA TAKASHI, TAKEICHI TSUBASA, EBDRUH SOREN, PETERSEN ANDERS KLARSKOV, WATANABE TAKASHI
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to a preparation method of a 7H-pyrrolo [2, 3-d] pyrimidine derivative and a synthetic intermediate thereof. The present invention provides processes for the preparation of 7H-pyrrolo [2, 3-d] pyrimidine derivatives useful as inhibitors of Janus Kinases (JAK), intermediates thereof, and processes for the preparation of the intermediates. The present invention provides a process for the preparation of 3-[(3S, 4R)-3-methyl-6-(7H-pyrrolo [2, 3-d] pyrimidin-4-yl)-1, 6-diazaspiro [3.4] octane-1-yl]-3-oxopropionitrile using a salt of (3S, 4R)-1-benzyl-3-methyl-1, 6-diazaspiro [3.4] octane and an organic acid, and a process for the preparation of 3-[(3S, 4R)-3-methyl-6-(7H-pyrrolo [2, 3-d] pyrimidin-4-yl)-1, 6-diazaspiro [3.4] octane-1-yl]-3-oxopropionitrile. 本发明涉及7H-吡咯并[2,3-d]嘧啶衍生物的制备方法及其合成中间体。本发明提供了作为詹纳斯激酶(JAK)抑制剂有用的7H-吡咯并[2,3-d]嘧啶衍生物的制备方法、其中间体和所述中间体的制备方法。本发明提供了使用(3S,4R)-1-苄基-3-甲基-1,6-二氮杂螺[3.4]辛烷与有机酸的盐来制备3-[(3S,4R)-3-甲基-6-(7H-吡咯并[2,3-d]嘧啶-4-基)-1,6-二氮杂螺[3.4]辛烷-1-基]-3-氧代丙腈的方法。