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1H-Pyrrolo[2,3-B]Pyridine 7-Oxide置于四甲基溴化铵,甲基磺酸酐体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 5.5H,反应生成 4-溴-7-氮杂吲哚
参考文献:通过铜催化的叠氮化物-炔烃环加成反应,溶液相平行合成鲁索替尼衍生的janus激酶抑制剂
标题:通过铜催化的叠氮化物-炔烃环加成反应,溶液相平行合成鲁索替尼衍生的janus激酶抑制剂
摘要:在当前的研究中开发了溶液相平行合成三唑衍生的ruxolitinib类似物.该方法利用铜催化的叠氮化物-炔烃环加成反应建立了中心三唑模板.通过沉淀和离心分离产物是直接的,并且产生适用于生物概况分析的高纯度化合物.建立了以高产率获得末端炔烃前体的简单方案,并制备了具有不同官能团的类索鲁替尼样三唑库.另外,提出了鲁索替尼与janus激酶(jak)2结合模式的模型.与以前的模型相比,该姿势解释了jak1 / Jak2的化合物选择性,并且与公开的结构活性数据一致.在此基础上,推导了用于逆转鲁索替尼选择性图谱的基于结构的设计假设.该策略的应用确定了对其他jak具有高选择性的中等效力的jak3抑制剂(35 Nm),可能利用了共价结合模式.
DOI:10.1021/co500122H

专利信息

专利号:US-2025179012-A1
优先权日:2022-03-04
标 题:Synthesis of sulfur(vi) compounds and reagents for same
发明人：LOPCHUK JUSTIN MATTHEW; SHULTZ ZACHARY
权利人:H LEE MOFFITT CANCER CT & RES
摘要:This disclosure provides reagents and processes for the synthesis of organic compounds, more particularly reagents and processes for the asymmetric synthesis of sulfur (VI) containing organic compounds.

专利号:WO-03000690-A1
优先权日:2001-06-25
标题:Synthesis of heterocyclic compounds employing microwave technology
发明人：MAJID TAHIR NADEEM; DEPRETS STEPHANIE D; PEDGRIFT BRIAN L
权利人:AVENTIS PHARMA INC; MAJID TAHIR NADEEM; DEPRETS STEPHANIE D; PEDGRIFT BRIAN L
摘要:This invention provides for processes for preparing compounds of the formula (I) comprising employing microwave energy.

专利号:WO-2021038419-A1
优先权日:2019-08-23
标题 :Kinase inhibitors and methods of synthesis and treatment
发明人：ZAVORONKOVS ALEKSANDRS; IVANENKOV YAN; POLYKOVSKIY DANIIL; ALIPER ALEKSANDR
权利人:INSILICO MEDICINE IP LTD
摘要:Compounds that function as kinase inhibitors are provided. The kinase inhibitors can have any structure of the formulae provided herein, such as shown for Compounds 1-4. A pharmaceutical composition can include: the compound of one of the embodiments; and a pharmaceutically acceptable carrier having the compound. A method of inhibiting a kinase can include: providing the compound of one of the embodiments described herein to the kinase such that the kinase is inhibited. The methods can include inhibiting DDR1 and/or DDR2, and thereby providing a modulation or decrease in the activity of DDR1 and/or DDR2. This decrease in DDR1 and/or DDR2 activity can be used as therapy to treat conditions related to DDR1 and/or DDR2 activity, such as fibrosis, cancer, and others.

专利号:EP-3103803-B1
优先权日:2008-10-27
标 题 :Intermediates for the synthesis of mtor kinase inhibitors

专利号:WO-2023168108-A2
优先权日:2022-03-04
标 题 :Synthesis of sulfur(vi) compounds and reagents for same

专利号:EP-3660020-A1
优先权日:2008-10-27
标题 :Process for the synthesis of mtor kinase inhibitors