CAS: 65673-63-4; Rel-(R)-Ethyl 2-Amino-6-Bromo-4-((R)-1-Cyano-2-Ethoxy-2-Oxoethyl)-4H-Chromene-3-Carboxylate(Relative)

该化合物是属于苯丙醚衍生物类别的化学化合物,具有一个复杂的分子结构,其特点是存在苯丙基,这是一个含有芳香和热循环成分的结合环系统;该化合物因其功能组群,溴亚基体和cyano组群等功能组而引人注目,这些功能组群有助于其再活性和潜在生物活动;该化学组群增强了其溶性,并可能影响其健康基因特性;由(R,4R)配置显示的立体化学结构结构结构显示,这些原子的具体空间安排能够影响化合物与生物目标的相互作用;

结构式图片

上下游产品

CAS号105-56-6 氰乙酸乙酯 | CAS号1761-61-1 5-溴水杨醛

合成工艺路线路线简述

  • 合成目标产物 Ha14-1 主要起始原料 Ethyl Cyanoacetate And 5-Bromosalicylaldehyde
  • (文献来源)合成步骤主要原料 Ethyl Cyanoacetate 和 5-Bromosalicylaldehyde

海关参考信息

专利信息


专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

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-6660871-B2
优先权日:2001-02-01
标 题 :Synthesis of 4H-chromene derivatives
发明人:HUANG ZIWEI
权利人:THOMAS JEFFERSON UNVERSITY
摘要:Substituted 4H-chromene derivatives are a new class of compounds that bind to Bcl-2 protein and induce apoptosis in tumor cells. The present invention is directed to an efficient synthetic method for the preparation of these compounds from salicylaldehyde derivatives and alkyl cyanoacetates under solid phase.

专利号:US-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人:KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.

专利号:CN-118922420-A
优先权日:2022-03-25
标题 :Synthesis of TYK2 inhibitors and their intermediates

供应商参考报价(招募中)

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: Niino S, Nakamura Y, Hirabayashi Y, Nagano-Ito M, Ichikawa S. A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase. Biochem Biophys Res Commun. 2013 Feb 26. doi:pii: S0006-291X(13)00312-4. 10.1016/j.bbrc.2013.02.052. [Epub ahead of print] doi: 10.1038/bjc.2011.604. Epub 2012 Jan 12.
4: Weyland M, Manero F, Paillard A, Grée D, Viault G, Jarnet D, Menei P, Juin P, Chourpa I, Benoit JP, Grée R, Garcion E. Mitochondrial targeting by use of lipid nanocapsules loaded with SV30, an analogue of the small-molecule Bcl-2 inhibitor HA14-1. J Control Release. 2011 Apr 10;151(1):74-82. doi: 10.1016/j.jconrel.2010.11.032. Epub 2010 Dec 5. doi: 10.1016/j.canlet.2009.11.014. Epub 2009 Dec 22. doi: 10.1158/1535-7163.MCT-09-0493. Epub 2009 Nov 3. doi: 10.1016/j.brainres.2009.05.097. Epub 2009 Jun 6.
8: Arisan ED, Kutuk O, Tezil T, Bodur C, Telci D, Basaga H. Small inhibitor of Bcl-2, HA14-1, selectively enhanced the apoptotic effect of cisplatin by modulating Bcl-2 family members in MDA-MB-231 breast cancer cells. Breast Cancer Res Treat. 2010 Jan;119(2):271-81. doi: 10.1007/s10549-009-0343-z. Epub 2009 Feb 24. doi: 10.1016/j.radonc.2008.08.006. Epub 2008 Sep 4. doi: 10.1111/j.1751-1097.2008.00371.x. Epub 2008 May 29.

合成参考文献


摘要:Xiao, X., Science of Synthesis: Knowledge Updates, (2023) 2, 242.
参考文献:10.1182/blood.v99.9.3461
摘要:Milella M, Estrov Z, Kornblau SM, Carter BZ, Konopleva M, Tari A, Schober WD, Harris D, Leysath CE, Lopez-Berestein G, Huang Z, Andreeff M. Synergistic induction of apoptosis by simultaneous disruption of the Bcl-2 and MEK/MAPK pathways in acute myelogenous leukemia. Blood. 2002 May 01;99(9):3461–4. doi: 10.1182/blood.v99.9.3461.
参考文献:10.1186/1756-9966-31-102
摘要:Li J, Li Y, Jin W, Yang Q, Shao Z, Tian X. ABT-737 reverses the acquired radioresistance of breast cancer cells by targeting Bcl-2 and Bcl-xL. Journal of Experimental & Clinical Cancer Research. 2012 Dec 23;31(1):102. doi: 10.1186/1756-9966-31-102.
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