CAS: 330786-24-8; 3-(4-Phenoxyphenyl)-1H-Pyrazolo[3,4-D]Pyrimidin-4-Amine

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CAS号2215-77-2 4-苯氧基苯甲酸 | CAS号330792-69-3 依鲁替尼中间体

4-苯氧基苯甲酸置于吡啶,氯化亚砜,N,N-二异丙基乙胺,N,N-二甲基甲酰胺体系中,用 甲苯 作为反应溶剂,化学反应 27.0H,反应生成 伊布替尼中间体n-2
参考文献:依鲁替尼中间体及其制备方法
标题:依鲁替尼中间体及其制备方法
摘要:本发明公开一种依鲁替尼中间体及其制备方法.本发明的依鲁替尼中间体,结构如式i所示,R的定义如说明书和权利要求书所示.本发明的依鲁替尼中间体可用于制备依鲁替尼关键中间体3‑(4‑苯氧基苯基)‑1H‑吡唑并[3,4‑d]嘧啶‑4‑胺,包括步骤:式i化合物在活性亲核试剂作用下制备得到活性中间体式ii化合物;式ii化合物经环化制备得到式4化合物3‑氨基‑5‑(4‑苯氧基苯基)‑4‑氰基‑1H‑吡唑;式4化合物经关环得到依鲁替尼关键中间体.本发明的方法原料便宜易得,不需要使用危险品试剂,反应条件温和,操作简单,适合工业化生产.

专利信息

专利号:US-2017327504-A1
优先权日:2014-10-30
标 题:Synthesis of Substituted 1H-Pyrazolo[3,4-D]Pyrimidines
发明人：ROSE CHRISTOPHER; SILBERGER HERBERT; SCHREINER ERWIN; FELZMANN WOLFGANG; MARAS NENAD
权利人:SANDOZ AG
摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.

专利号:US-2019040070-A1
优先权日:2016-02-09
标 题:Process for the synthesis of stable amorphous ibrutinib
发明人：MAIER THOMAS; KARAPETYAN INNA; ARAKELYAN ALVARD; MARGARYAN TAMARA; SARGSYAN VARDAN; STEPANYAN HEGHINE; ABOVYAN HERMINE; GERBER AESCHBACHER ROMAN; HAFERKAMP SVEN
权利人:AZAD PHARMACEUTICAL INGREDIENTS AG
摘要:Disclosed herein is a new route of synthesis and a new stable amorphous form of ibrutinib. Also disclosed are pharmaceutical compositions, oral dosage forms and the use of the amorphous ibrutinib in the treatment of mantle cell lymphoma or chronic lymphocytic leukemia.

专利号:WO-2020117135-A1
优先权日:2018-12-04
标 题:A process for preparation of 1h-pyrazolo[3,4-d] pyrimidine derivatives
发明人：HAAS PHILIPP DANIEL; STECKEL ANDREAS HARTWIG; BELLUR ATICI ESEN; ALTUNDAS RAMAZAN; OZTURK AYDIN BUSRA; SECEN HASAN; AYDIN BUSRA NUR
权利人:DEVA HOLDING AS
摘要:The present invention relates to an efficient and industrially advantageous process for the preparation of 1H-pyrazolo[3,4-d] pyrimidine derivatives. In particular the present invention provides a process for the preparation of 4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4- d]pyrimidine and tert-butyl (R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4- d]pyrimidin-1-yl)piperidine-1-carboxylate. Said compounds are important intermediates in the synthesis of ibrutinib. The method provided for preparing intermediates of ibrutinib has the advantages of a simple operation, high yield and low costs.

专利号:US-2018282336-A1
优先权日:2014-10-30
标题:Active Acrylamides
发明人：FELZMANN WOLFGANG; BRUNNER STEFANIE; LENGAUER HANNES
权利人:SANDOZ AG
摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds, which are used as a masked form of acrylamides and in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (ibrutinib) and its synthesis intermediates.

专利号:WO-2017137446-A1
优先权日:2016-02-09
标题:Process for the synthesis of stable amorphous ibrutinib

专利号:EP-3414248-A1
优先权日:2016-02-09
标题 :Process for the synthesis of stable amorphous ibrutinib