CAS: 934526-89-3; 2-Amino-N-(3-(N-(3-((2-Chloro-5-Methoxyphenyl)Amino)Quinoxalin-2-yl)Sulfamoyl)Phenyl)-2-Methylpropanamide

该化合物是磷酸三基酶(PI3K)路径的选择性抑制剂, 具体针对异族体(PI3K) . 该化合物主要因其在肿瘤和自体免疫性疾病中的潜在治疗应用而受到调查, 因为PI3K路径在细胞生长,扩散和存活方面发挥着关键作用. Pilaralisib 展示了一种有利的药用植物基因特征,允许口服,并在各种临床试验中进行了研究,以评估其在治疗淋巴瘤和其他血病恶性肿瘤等病的疗效和安全性.其行动机制包括抑制PI3K, 主要是在白细胞病中表现, 从而调节免疫反应和肿瘤生长. 与许多有针对性的疗法一样, Pilaralisib 的研制工作也伴随着对生物标志的研究, 从而可以预测病人的反应, 加强治疗中的个人化医学方法. 总的来说, Pilaralisib 代表了癌症治疗领域目标疗法的研制过程中的重大进展.

结构式图片

物理性质

MSDS等安全信息

欧盟法规

C&L通报

上下游产品

N-(3-((2-Chloro-5-Methoxyphenyl)Amino)Quinoxalin-2-yl)-3-Nitrobenzenesulfonamide 934528-15-1
(N-(3-Chloroquinoxalin-2-yl)-3-Nitrobenzenesulfonamide) 731815-55-7

合成工艺路线路线简述

  • 合成目标产物 Pilaralisib 主要起始原料 2,3-Dichloroquinoxaline
  • 59660-95-6 + 1433222-74-2 = 934526-89-3
    反应条件:1.1 Solvents: Dimethylformamide; 5 °C -> 50 °C1.2 Reagents: Dipotassium Phosphate Solvents: Ethanol,Water; 50 °C -> 10 °C; 2 H,0 °C
    标题:Phosphatidylinositol 3-Kinase Inhibitors For The Treatment Of Childhood Cancers
    参考文献:World Intellectual Property Organization]

    59660-95-6 + 1433222-74-2 = 934526-89-3
    反应条件:1.1 Solvents: Dimethylformamide; 5 °C -> 50 °C1.2 Reagents: Dipotassium Phosphate Solvents: Ethanol,Water; 50 °C -> 10 °C; 2 H,10 °C
    标题:N- (3-{[(3-{[2-Chloro-5-(Methoxy) Phenyl]Amino} Quinoxalin-2-Yl) Amino]Sulfonyl} Phenyl)-2-Methylalaninamide As Phosphatidylinositol 3 - Kinase Inhibitor For The Treatment Of Lymphoproliferative Malignancies
    参考文献:World Intellectual Property Organization]

    30992-29-1 = 934526-89-3
    反应条件:1.1 Reagents: Diisopropylethylamine,O-(7-Azabenzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Hexafluorophosphate Solvents: Dimethylformamide; Overnight,Rt1.2 Reagents: Hydrochloric Acid Solvents: 1,4-Dioxane; 3 H,Rt
    标题:Preparation Of N-(Quinoxalin-2-Yl) Benzenesulfonamides As Phosphatidylinositol 3-Kinase Inhibitors
    参考文献:World Intellectual Property Organization]

    = 934526-89-3 [标题:Reaction Conditions
    标题:A Tablet Formulation Of A Pi3K Inhibitor For Cancer Treatment
    参考文献:World Intellectual Property Organization]

    = 934526-89-3 [标题:Reaction Conditions
    标题:Compounds For Use In The Treatment Of Basal Cell Carcinoma
    参考文献:World Intellectual Property Organization]

    = 934526-89-3 [标题:Reaction Conditions
    标题:Quinaxoline Derivatives As Inhibitors Of Pi3K-Alpha And Their Preparation,Pharmaceutical Compositions And Use In The Treatment Of Cancer
    参考文献:World Intellectual Property Organization]

    5938-34-1 = 934526-89-3
    反应条件:1.1 Solvents: Dimethylformamide; 5 °C; 5 °C -> 50 °C1.2 Reagents: Dipotassium Phosphate Solvents: Ethanol,Water; 50 °C -> 10 °C; 2 H,10 °C
    标题:Phosphatidylinositol 3-Kinase Inhibitors For The Treatment Of Cancer
    参考文献:World Intellectual Property Organization]

    30992-29-1 = 934526-89-3
    反应条件:1.1 Reagents: Diisopropylethylamine,O-(7-Azabenzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Hexafluorophosphate Solvents: Dimethylformamide; Overnight,Rt1.2 Reagents: Hydrochloric Acid Solvents: 1,4-Dioxane; 3 H,Rt
    标题:Combinations Of Kinase Inhibitors For The Treatment Of Cancer
    参考文献:World Intellectual Property Organization]

    75-64-9 = 934526-89-3
    反应条件:1.1 Reagents: Diisopropylethylamine,O-(7-Azabenzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Hexafluorophosphate Solvents: Dimethylformamide,Dichloromethane; Overnight,Rt
    标题:2-Amino-3-Sulfonylaminoquinoxaline Derivatives As Phosphatidylinositol 3-Kinase Inhibitors And Their Preparation,Pharmaceutical Compositions And Use In The Treatment Of Cancer
    参考文献:World Intellectual Property Organization]

    = 934526-89-3 [标题:Reaction Conditions
    标题:Preparation Of Anticancer Agents Modified By Maleimide Derivatives As Protein-Binding Drugs For Treatment Of Cancers
    参考文献:World Intellectual Property Organization]

    = 934526-89-3 [标题:Reaction Conditions
    标题:Formulation Of Tablet Of An Inhibitor Of Phosphatidylinositol 3-Kinase For Cancer Treatment
    参考文献:France]

    = 934526-89-3 [标题:Reaction Conditions
    标题:Pyrimidine Derivatives As Jak-2 Inhibitors In Combination With Other Agents And Their Preparation And Use In The Treatment Of Diseases
    参考文献:World Intellectual Property Organization]

    = 934526-89-3 [标题:Reaction Conditions
    标题:Preparation Of Azetidine Mek Kinase Inhibitors And Pyridopyrimidine And Quinoxaline And Analog Pi3K Inhibitors And Methods Of Using Mek Inhibitors In Combination With Pi3K Inhibitors For The Treatment Of Proliferative Diseases,Especially Cancer
    参考文献:World Intellectual Property Organization
📜(N-(3-Chloroquinoxalin-2-yl)-3-Nitrobenzenesulfonamide)置于platinum Sulfide On Carbon,Potassium Formate,1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 四氢呋喃,乙醇,水,乙腈 作为反应溶剂,化学反应 2.0H,反应生成 2-氨基-N-[3-[n-[3-[(2-氯-5-甲氧基苯基)氨基]喹喔啉-2-基]氨基磺酰基]苯基]-2-甲基丙酰胺
参考文献:Phosphatidylinositol 3-Kinase Inhibitors For The Treatment Of Lymphoproliferative Malignancies
标题:Phosphatidylinositol 3-Kinase Inhibitors For The Treatment Of Lymphoproliferative Malignancies
摘要:提供了一种治疗淋巴增生性恶性肿瘤的方法,适用于需要此类治疗的患者,包括向患者施用本文所述的化合物a的有效量.

海关参考信息

专利信息


专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人：ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-10772971-B2
优先权日:2017-06-22
标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
发明人：GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

专利号:US-10906888-B2
优先权日:2016-07-14
标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
发明人：CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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主要参考文献


1: Shah N, Mohammad AS, Saralkar P, Sprowls SA, Vickers SD, John D, Tallman RM, Lucke-Wold BP, Jarrell KE, Pinti M, Nolan RL, Lockman PR. Investigational chemotherapy and novel pharmacokinetic mechanisms for the treatment of breast cancer brain metastases. Pharmacol Res. 2018 Jun;132:47-68. doi: 10.1016/j.phrs.2018.03.021. Epub 2018 Mar 28.
2: Zhou J, Wang Y, Zhu G, Yan M, Li Z, Li L, Kuang J, Zhang W, Huang C, Ren F, Yang Q. Pilaralisib inhibits the replication of enteroviruses by targeting the PI3K/AKT signaling pathway. Virol J. 2025 Jul 28;22(1):257. doi: 10.1186/s12985-025-02881-w.
3: Edelman G, Rodon J, Lager J, Castell C, Jiang J, Van Allen EM, Wagle N, Lindeman NI, Sholl LM, Shapiro GI. Phase I Trial of a Tablet Formulation of Pilaralisib, a Pan-Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors. Oncologist. 2018 Apr;23(4):401-e38. doi: 10.1634/theoncologist.2017-0691. Epub 2018 Mar 28.

合成参考文献


参考文献:10.1007/s10549-015-3615-9
摘要:Blackwell K, Burris H, Gomez P, Lynn Henry N, Isakoff S, Campana F, Gao L, Jiang J, Macé S, Tolaney SM. Phase I/II dose-escalation study of PI3K inhibitors pilaralisib or voxtalisib in combination with letrozole in patients with hormone-receptor-positive and HER2-negative metastatic breast cancer refractory to a non-steroidal aromatase inhibitor. Breast Cancer Research and Treatment. 2015 Oct 24;154(2):287–97. doi: 10.1007/s10549-015-3615-9.
参考文献:10.1186/s11658-018-0088-y
摘要:Gwangwa MV, Joubert AM, Visagie MH. Crosstalk between the Warburg effect, redox regulation and autophagy induction in tumourigenesis. Cellular & Molecular Biology Letters. 2018 May 04;23(1):20. doi: 10.1186/s11658-018-0088-y.
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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