JAK INHIBITOR, AND MANUFACTURING METHOD OF RELATED INTERMEDIATE COMPOUND

• Main Authors: XIA MICHAEL, LIU PINGLI, LIN QIYAN, METCALF BRIAN W, MELONI DAVID, PAN YONGCHUN, YUE TAI-YUEN, ZHOU JIACHENG, MEI LI, WANG HAISHENG, RODGERS JAMES D
• Format: Patent
• Language: English; Japanese
• Published: 14.05.2020
• Subjects: CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOIDCHEMISTRY; CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY; PERFORMING OPERATIONS; PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL; THEIR RELEVANT APPARATUS; TRANSPORTING

To provide chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidine useful as a JAK inhibitor for treatments of inflammatory diseases, bone marrow proliferative disorders or the like.SOLUTION: There is provided a manufacturing method of a compound XII, including: reacting a compound X with XIII in presence of a palladium catalyst, a base and a solvent, and forming XII. In the formula Xis tosylate, triflate, I, Cl or Br; Rand Rare independently H or Calkyl, or Rand Rare together with O to which they bind, or B to which O binds to form a 5 to 6-membered heterocyclic ring, the heterocyclic ring is optionally substituted by 1 to 4 Calkyl groups; and Pand Pare independently a protective group.SELECTED DRAWING: None 【課題】炎症性疾患、骨髄増殖性障害等の治療のためのＪＡＫ阻害剤として有用なキラル置換ピラゾリルピロロ［２，３−ｄ］ピリミジンの提供。【解決手段】化合物ＸＩＩの製造方法であって、パラジウム触媒、塩基および溶媒の存在下で、化合物ＸをＸＩＩＩと反応させて、ＸＩＩを形成することを包含する方法（式中、Ｘ２は、トシラート、トリフラート、Ｉ、ＣｌまたはＢｒ；ＲｃとＲｄは、独立して、ＨまたはＣ１−６アルキル；あるいはＲｃおよびＲｄは、それらが結合されるＯならびにＯが結合されるＢと一緒になって、５〜６員複素環を形成して、その複素環は、１〜４個のＣ１−４アルキル基で任意に置換され；Ｐ１およびＰ２は、独立して、保護基である）。【選択図】なし