CAS: 1382979-44-3; 5-(6,6-Dimethyl-4-Morpholino-8,9-Dihydro-6H-[1,4]Oxazino[4,3-E]Purin-2-yl)Pyrimidin-2-Amine

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上下游产品

2-Chloro-6,6-Dimethyl-4-Morpholino-8,9-Dihydro-6H-[1,4]Oxazino[4,3-E]Purine 1382980-58-6
2-(2-Chloro-6-Morpholino-9-(Tetrahydro-2H-Pyran-2-yl)-9H-Purin-8-yl)Propan-2-Ol 1198171-66-2
2-(2-氯-6-吗啉代-9H-嘌呤-8-基)丙-2-醇 2-(2-Chloro-6-Morpholino-9H-Purin-8-yl)Propan-2-Ol 1198171-62-8
2-Chloro-6-(Morpholin-4-yl)-9-(Tetrahydro-2H-Pyran-2-yl)-9H-Purine 95758-04-6

合成工艺路线路线简述

    📜2-Chloro-6-(Morpholin-4-yl)-9-(Tetrahydro-2H-Pyran-2-yl)-9H-Purine置于盐酸,正丁基锂,Potassium Phosphate Monohydrate,Xphos Pd G2,异丙基氯化镁,Potassium Carbonate体系中,用 四氢呋喃,甲醇,正己烷,水 用作溶剂,化学反应 20.5H,反应生成5-[8,9-二氢-6,6-二甲基-4-(4-吗啉基)-6H-[1,4]恶嗪并[4,3-E]嘌呤-2-基]-2-嘧啶胺
    参考文献:Development Of An Efficient,Safe,And Environmentally Friendly Process For The Manufacture Of Gdc-0084
    标题:Development Of An Efficient,Safe,And Environmentally Friendly Process For The Manufacture Of Gdc-0084
    摘要:An Improved,Efficient Process With A Significantly Reduced Process Mass Intensity (Pmi) Led To The Multikilogram Synthesis Of A Brain Penetrant Pi3K Inhibitor Gdc-0084. Highlights Of The Synthesis Include A Phase Transfer Catalyzed Annulation In Water,An Efficient Suzuki-Miyaura Cross-Coupling Of A Chloropyrimidine With An Arylboronic Acid Using A Low Palladium Catalyst Loading,And The Development Of A Controlled Crystallization To Provide The Api. The Process Delivered Gdc-0084 With Low Levels Of Both Impurities And Residual Metals.
    Doi:10.1021/acs.Oprd.6B00011

    海关参考信息

    专利信息


    专利号:US-11434195-B2
    优先权日:2017-07-20
    标题:Compositions and methods for treatment of central nervous system tumors
    发明人:SVETLOV STANISLAV IGOREVICH
    权利人:UNIV FLORIDA
    摘要:Compounds, pharmaceutical compositions, and methods for treating cancer, in particular brain cancer, are provided, including amphiphilic fatty acid/alcohol ethers (AIPs) comprising endocannabinoid and FABP motifs covalently linked to a beta-adrenoreceptor antagonist motif in one molecule. The invention includes methods for inhibiting growth of brain cancer cells by contacting the compound(s) with brain cancer cells. The invention provides a method for treating both brain cancer and brain cancer metastases, and for suppression of regrowth of brain cancer cells after radiation, surgical treatment, or chemotherapy of brain cancer. The invention also comprises an optimized chemical synthesis of the AIP compounds and methods of using the compounds, alone or in combination with another agent, for suppressing the growth of brain cancer cells, and enhancing survival of normal CNS cells, or improving recuperation from radiation, surgical or chemotherapy.

    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.

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    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Salphati L, Alicke B, Heffron TP, Shahidi-Latham S, Nishimura M, Cao T, Carano RA, Cheong J, Greve J, Koeppen H, Lau S, Lee LB, Nannini-Pepe M, Pang J, Plise EG, Quiason C, Rangell L, Zhang X, Gould SE, Phillips HS, Olivero AG. Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma. Drug Metab Dispos. 2016 Dec;44(12):1881-1889. Epub 2016 Sep 16. doi: 10.1021/acsmedchemlett.6b00005. eCollection 2016 Apr 14.

    合成参考文献


    参考文献:10.1158/1078-0432.ccr-19-2808
    摘要:Wen PY, Cloughesy TF, Olivero AG, Morrissey KM, Wilson TR, Lu X, Mueller LU, Coimbra AF, Ellingson BM, Gerstner E, Lee EQ, Rodon J. First-in-Human Phase I Study to Evaluate the Brain-Penetrant PI3K/mTOR Inhibitor GDC-0084 in Patients with Progressive or Recurrent High-Grade Glioma. Clin Cancer Res. 2020 Apr 15;26(8):1820–8. doi: 10.1158/1078-0432.ccr-19-2808.
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