CAS: 1513857-77-6; 3-(2,6-Difluoro-3,5-Dimethoxyphenyl)-1-Ethyl-8-(Morpholinomethyl)-1,3,4,6-Tetrahydro-2H-Pyrrolo[3',2':5,6]Pyrido[4,3-D]Pyrimidin-2-One

结构式图片

上下游产品

3-(2,6-Difluoro-3,5-Dimethoxyphenyl)-1-Ethyl-1,3,4,7-Tetrahydro-2H-Pyrrolo[3',2':5,6]Pyrido[4,3-D]Pyrimidin-2-One 1513857-72-1
3-(2,6-Difluoro-3,5-Dimethoxyphenyl)-1-Ethyl-8-(Morpholin-4-Ylmethyl)-7-(Phenylsulfonyl)-1,3,4,7-Tetrahydro-2H-Pyrrolo[3',2':5,6]Pyrido[4,3-D]Pyrimidin-2-One 1513860-02-0
3-(2,6-Difluoro-3,5-Dimethoxyphenyl)-1-Ethyl-2-Oxo-7-(Phenylsulfonyl)-2,3,4,7-Tetrahydro-1H-Pyrrolo[3',2':5,6]Pyrido[4,3-D]Pyrimidine-8-Carbaldehyde
3-(2,6-Difluoro-3,5-Dimethoxyphenyl)-1-Ethyl-7-(Phenylsulfonyl)-1,3,4,7-Tetrahydro-2H-Pyrrolo[3',2':5,6]Pyrido[4,3-D]Pyrimidin-2-One 1513860-01-9
5-{[(2,6-Difluoro-3,5-Dimethoxyphenyl)Amino]Methyl}-N-Ethyl-1H-Pyrrolo[2,3-B]Pyridin-4-Amine 1513859-26-1

合成工艺路线路线简述

  • 合成目标产物 Pemigatinib 主要起始原料 4-Chloro-1H-Pyrrolo[2,3-B]Pyridine-5-Carbaldehyde
  • (文献来源)合成步骤主要原料 4-Chloro-1H-Pyrrolo[2,3-B]Pyridine-5-Carbaldehyde
4-(Ethylamino)-1H-Pyrrolo[2,3-B]Pyridine-5-Carbaldehyde置于四丁基氟化铵,Sodium Hydride,(1S)-(+)-10-Camphorsulfonic Acid,溶剂黄146,Lithium Diisopropyl Amide体系中,用 四氢呋喃,5,5-Dimethyl-1,3-Cyclohexadiene,二氯甲烷,N,N-二甲基甲酰胺,Mineral Oil 用作溶剂,化学反应 64.5H,反应生成培米加替尼
参考文献:发现 Pemigatinib:一种有效且选择性的成纤维细胞生长因子受体 (Fgfr) 抑制剂
标题:发现 Pemigatinib:一种有效且选择性的成纤维细胞生长因子受体 (Fgfr) 抑制剂
摘要:Fgfr 的异常激活与许多肿瘤类型的发病机制有关.Fgfr 的选择性抑制已成为一种有前途的癌症治疗方法.在此,我们描述了化合物38(incb054828,Pemigatinib)的发现,该化合物是 Fgfr1,Fgfr2 和 Fgfr3 的高效选择性抑制剂,具有优异的理化特性和药代动力学特征.Pemigatinib 已获得美国食品和药物管理局的加速批准,用于治疗患有 Fgfr2 融合或其他重排的先前治疗过的,不可切除的局部晚期或转移性胆管癌的成人.其他临床试验正在进行中,以在 Fgfr 改变的患者中评估 Pemigatinib.
Doi:10.1021/acs.Jmedchem.1C00713

海关参考信息

专利信息


专利号:US-6133409-A
优先权日:1996-12-19
标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds
发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARM PROD INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

专利号:US-3959322-A
优先权日:1960-09-22
标 题:Synthesis of 13-alkyl-gon-4-ones
发明人:HUGHES GORDON ALAN; SMITH HERCHEL
权利人:SMITH HERCHEL
摘要:The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.

专利号:US-6229055-B1
优先权日:1996-04-12
标题 :Synthesis of fluorinated xanthene derivatives
发明人:KLAUBERT DIETER H; GEE KYLE R
权利人:MOLECULAR PROBES INC
摘要:Facile syntheses for fluorinated resorcinol and aminophenol derivatives are provided that yield isomer-free products in good yield. These novel methods use generally available precursors and standard laboratory reagents and equipment to reproducibly produce these synthetically useful reagents in relatively large quantities. The resulting fluorinated resorcinols and aniinophenols possess utility in the preparation of fluorinated fluorescein and rhodol dyes.

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

专利号:US-7417142-B2
优先权日:2002-03-28
标 题:Chiral porphyrins, chiral metalloporphyrins, and methods for synthesis of the same
发明人:ZHANG X PETER; CHEN YING; GAO GUANG-YAO
权利人:UNIV TENNESSEE RES FOUNDATION
摘要:Novel methods of synthesizing heteroatom-containing chiral porphyrins and chiral metalloporphyrins and the novel chiral porphyrins and chiral metalloporphyrins themselves are disclosed. Metal complexes of the chiral porphyrins are prepared in high yields and shown to be active catalysts for highly enantioselective and diastereoselective cyclopropanation, aziridination, and epoxidation of alkenes under a practical one-pot protocol.

专利号:US-7722851-B2
优先权日:2001-12-10
标题 :Bulk synthesis of carbon nanotubes from metallic and ethynyl compounds
发明人:KELLER TEDDY M; QADRI SYED B
权利人:US NAVY
摘要:A process of making carbon nanotubes comprising the steps of: providing a precursor composition comprising at least one metallic compound and at least one organic compound; wherein the organic compound is selected from the group consisting of an ethynyl compound, a metal-ethynyl complex, and combinations thereof; wherein the precursor composition is a liquid or solid at room temperature; and heating the precursor composition under conditions effective to produce carbon nanotubes. A carbon nanotube composition comprising carbon nanotubes and a metal component selected from the group consisting of metal nanoparticles and elemental metal; wherein the carbon nanotube composition is rigid.
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主要参考文献


1: Gnagni L, Ruscito I, Zizzari IG, Nuti M, Napoletano C, Rughetti A. Precision oncology targeting FGFRs: A systematic review on pre-clinical activity and clinical outcomes of pemigatinib. Crit Rev Oncol Hematol. 2024 Jul 31;202:104464. doi: 10.1016/j.critrevonc.2024.104464. Epub ahead of print. 9(7):103625. doi: 10.1016/j.esmoop.2024.103625. Epub 2024 Jul 9.
3: Kaneko J, Kiuchi R, Takinami M, Ohnishi I, Ito J, Jindo O, Nishino M, Takahashi Y, Yamada T, Sakaguchi T. Successful intrahepatic cholangiocarcinoma conversion surgery after administration of fibroblast growth factor receptor inhibitor. Clin J Gastroenterol. 2024 Jul 10. doi: 10.1007/s12328-024-02014-w. Epub ahead of print.
3:1247296. doi: 10.3389/fopht.2023.1247296.

合成参考文献


参考文献:10.1038/s41419-020-02896-x
摘要:Zhu H, Zhai B, He C, Li Z, Gao H, Niu Z, Jiang X, Lu J, Sun X. LncRNA TTN-AS1 promotes the progression of cholangiocarcinoma via the miR-320a/neuropilin-1 axis. Cell Death & Disease. 2020 Aug 15;11(8):637. doi: 10.1038/s41419-020-02896-x.
参考文献:10.1007/s12029-021-00637-7
摘要:Huang P, Zhou Y, Chen Y. Significant Response to Camrelizumab Plus Targeted Drugs in Recurrent Intrahepatic Cholangiocarcinoma: a Case Report and Literature Review. Journal of Gastrointestinal Cancer. 2021 Jul 26;53(3):817–24. doi: 10.1007/s12029-021-00637-7.
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