CAS: 244240-24-2; (Z)-2-Yano-N-(2,5-Dibromophenyl)-3-Hydroxybut-2-Enamide

上下游产品

N-(2,5-dibromophenyl)-2-cyanoacetamide acetyl chloride acetic anhydride 2,5-dibromoaniline

📜2,5-二溴苯胺置于sodium Hydride,达卡巴嗪体系中,用 四氢呋喃 用作溶剂,化学反应生成(2Z)-2-氰基-N-(2,5-二溴苯基)-3-羟基-2-丁烯酰胺
参考文献:对取代来氟米特固态分子间/分子内氢键的结构影响:X射线晶体结构的证据
标题:对取代来氟米特固态分子间/分子内氢键的结构影响:X射线晶体结构的证据
摘要:我们报告了九种取代的来氟米特代谢物类似物 (Lfm) 的 X 射线晶体结构研究结果.比较这些结构不同的 Lfm 类似物所表现出的氢键特性,特别有助于了解单个化合物晶体结构中存在的分子间和分子内氢键模式.所有化合物都具有很强的分子内氢键.此外,除 2,5-二氟苯基取代的 Lfm 类似物外,所有其他化合物均与卤素原子和 Nh 基团形成分子间或分子内氢键.然而,我们发现在 2,5-二氟和 2-氟衍生物的苯环 2-位存在氟原子导致结构骨架中只有一个分子内氢键.反之,3,5-二氟取代的 Lfm 类似物具有与其他卤化物取代的衍生物共有的分子内氢键.2,5-二氟和2-氟取代的化合物表现出的异常可能是由于与其他类似物结构中的氯和溴原子相比,氟原子的尺寸较小.由于这些分子的晶体堆积不同,在苯环的 2-位存在氟可能会破坏在其他衍生物中观测到的分子间氢键.5-二氟和2-氟取代的化合物可能是由于与其他类似物结构中
Doi:10.1016/j.Molstruc.2005.02.024

专利信息

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-2015217006-A1
优先权日:2014-02-06
标题:Al-f-18-labeled, al-f-19-labeled and ga-68-labeled gastrin-releasing peptide receptor (grpr)-antagonists for imaging of prostate cancer
发明人：MCBRIDE WILLIAM J; CHATALIC KRISTELL L S; HENDRIKS-DE JONG MARION; BOERMAN OTTO C; GOLDENBERG DAVID M
权利人:IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of 18 F-, 19 F- or 68 Ga-labeled molecules of use in PET, SPECT and/or MRI imaging of prostate cancer. Preferably, the 18 F, 19 F or 68 Ga is attached to a chelator moiety on a prostate cancer targeting molecule, more preferably a bombesin analog, more preferably a GRPR antagonist, most preferably JMV5132 or JMV4168. The 18 F or 19 F may form a complex with a group IIIA metal to promote binding to the chelators. The labeled molecules may be used to detect, diagnose and/or image prostate cancer, including metastatic prostate cancer, in vivo.

专利号:US-2016045626-A1
优先权日:2007-01-11
标题 :Methods and Compositions for Improved Labeling of Targeting Peptides
发明人：MCBRIDE WILLIAM J; GOLDENBERG DAVID M
权利人:IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of labeled targeting peptides, such as octreotide, octreotate, or other somatostatin analogs or derivatives. The targeting peptide may be labeled with a therapeutic or diagnostic isotope, such as 61 Cu, 62 Cu, 64 Cu, 67 Cu, 18 F, 19 F, 66 Ga, 67 Ga, 68 Ga, 72 Ga, 111 In, 177 Lu, 44 Sc, 47 Sc, 86 Y, 88 Y, 90 Y, 45 Ti or 89 Zr, preferably 18 F or 19 F. More preferably, the targeting peptide is NOTA-octreotate, NOTA-MPAA-octreotate, pyridine-NOTA-octreotate or triazole-NOTA-octreotate. The labeled targeting peptides may be used for detection, diagnosis, imaging and/or treatment of sst 2 + tumors, such as neuroendocrine tumors.

专利号:US-9150522-B2
优先权日:2011-10-25
标 题:Kinase inhibitor and method for treatment of related diseases
发明人：PAN ZHENGYING; LI XITAO
权利人:UNIV PEKING SHENZHEN GRAD SCHO; BEIJING RECIPROCAPHARMACEUTICALS CO LTD
摘要:Disclosed is a compound of (aminophenylamino) pyrimidyl benzamides and a synthesis method thereof. The compound has Btk-inhibition activity and can be used to treat autoimmune diseases, heteroimmune diseases, cancers or thromboembolic diseases.

专利号:US-2025049968-A1
优先权日:2022-04-21
标 题 :Therapeutic and imaging agents for targeting myocardial tissue
发明人：EEDA VENKATESWARARAO; AWASTHI VIBHUDUTTA
权利人:UNIV OKLAHOMA
摘要:Analogs and derivatives of omecamtiv mecarbil (OM), including an 18F-labeled analog, and methods of synthesis thereof. Cardiac myosin targeting vectors comprising a lipid anchoring/solubilizing moiety conjugated to a head made of OM or the OM analog or derivative. Liposomes comprising a cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of treating a cardiac condition or disease in a subject by administering to the subject the cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of synthesizing an 18F-labeled analog of OM.