CAS: 1029044-16-3; 5-((5-Chloro-1H-Pyrrolo[2,3-B]Pyridin-3-yl)Methyl)-N-((6-(Trifluoromethyl)Pyridin-3-yl)Methyl)Pyridin-2-Amine

上下游产品

tert-butyl N-[(tert-butoxy)carbonyl]-N-(5-formylpyridin-2-yl)carbamate 5-chloro-1H-pyrrolo[2,3-b]pyridine 23H27ClN4O5C23H27ClN4O5 6-(trifluoromethyl)pyridine-3-carbaldehyde

2-氨基-3-溴-5-氯吡啶置于盐酸,三乙基硅烷,甲基氯化镁,Palladium Diacetate,N,N-二异丙基乙胺,三(邻甲基苯基)磷,三氟乙酸,Potassium Hydroxide体系中,用 四氢呋喃,甲醇,二甲胺,乙腈 用作溶剂,化学反应 120.5H,反应生成培西达替尼
参考文献:通过串联tsuji-Trost反应和heck偶联探索pexidartinib的探索性工艺开发
标题:通过串联tsuji-Trost反应和heck偶联探索pexidartinib的探索性工艺开发
摘要:抽象的 设计并证明了一种新的合成途径来合成csf1R抑制剂pexidartinib.成功合成的关键是串联的tsuji-Trost反应和与钯和银催化结合的heck偶联.通过五个步骤以49%的收率获得最终产物,纯度高达99.2%.廉价和可用的材料和试剂以及易于进行后处理和纯化的操作使该路线更加实用. 设计并证明了一种新的合成途径来合成csf1R抑制剂pexidartinib.成功合成的关键是串联的tsuji-Trost反应和与钯和银催化结合的heck偶联.通过五个步骤以49%的收率获得最终产物,纯度高达99.2%.廉价和可用的材料和试剂以及易于进行后处理和纯化的操作使该路线更加实用.
Doi:10.1055/s-0037-1612421

专利信息

专利号:US-9745298-B2
优先权日:2015-05-06
标题:Synthesis of a compound that modulates kinases
发明人：IBRAHIM PRABHA N; JIN MASAYOSHI; MATSUURA SHINJI
权利人:PLEXXIKON INC; DAIICHI SANKYO CO LTD
摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nor a salt thereof, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

专利号:US-2022259212-A1
优先权日:2019-07-11
标题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase
发明人：BOSS CHRISTOPH; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in the treatment of inter alia cancer is disclosed.

专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人：EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

专利号:US-2025082766-A1
优先权日:2022-03-31
标 题 :Treatment of brain tumors by targeting the cholesterol pathway in astrocyes
发明人：MAYO LIOR
权利人:UNIV RAMOT
摘要:A method of treating a brain tumor in a subject in need thereof is disclosed. The method comprising administering to the subject a therapeutically effective amount of an agent capable of downregulating activity or expression of a component of the lipid synthesis and/or transportation pathways in an astrocyte in the tumor microenvironment and/or a therapeutically effective amount of a molecule which is associated with lipid uptake by the tumor cells or immune cells in the tumor microenvironment, or a polynucleotide encoding same.

专利号:US-2018305358-A1
优先权日:2015-05-06
标 题:Synthesis of a compound that modulates kinases

专利号:US-10399975-B2
优先权日:2015-05-06
标题:Synthesis of a compound that modulates kinases