CAS: 27035-30-9; Oxametacin

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CAS号20357-37-3 1-(4-Chlorobenz... | CAS号53-86-1 吲哚美辛

📜吲哚美辛置于n,N'-羰基二咪唑,盐酸羟胺体系中,用 四氢呋喃 用作溶剂,化学反应 1.0H,反应生成奥沙美辛
参考文献:1,4,2-二恶唑-5-酮对烯烃进行硫醚导向的nih催化远程γ-C(Sp3)-H加氢酰胺化
标题:1,4,2-二恶唑-5-酮对烯烃进行硫醚导向的nih催化远程γ-C(Sp3)-H加氢酰胺化
摘要:开发了一种 Nih 催化的硫醚导向的环金属化策略,以实现未活化烯烃的远程亚甲基 C-H 键酰胺化.由于优先形成五元镍环,由 Nih 插入烯烃引发的链式异构化可以在远离烯烃部分的 γ-亚甲基位点终止.通过使用 2,9-二丁基-1,10-菲咯啉 ( L4 ) 作为配体和二恶唑酮作为试剂,酰胺化发生在 γ-C(Sp 3 )-H 键上,以提供高达 90% 的酰胺产物产量(> 40 个例子)具有显着的区域选择性(高达 24:1 Rr).
Doi:10.1021/jacs.1C05834

专利信息

专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人：BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:AU-2022276509-A1
优先权日:2021-05-20
标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

专利号:US-9994558-B2
优先权日:2013-09-20
标题 :Multicyclic compounds and methods of using same
发明人：BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).

专利号:WO-2022246227-A1
优先权日:2021-05-20
标 题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

专利号:WO-2011011384-A9
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates