CAS: 55300-29-3; 2-[4-[3-(Trifluoromethyl)Phenyl]Piperazin-1-Yl]Ethyl 2-[[7-(Trifluoromethyl)Quinolin-4-Yl]Amino]Benzoate

📜4-[3-(三氟甲基)苯基]-1-哌嗪乙醇置于4-二甲氨基吡啶,Iron(Iii) Chloride,Lithium Chloro-Isopropyl-Magnesium Chloride,三乙胺体系中,用 四氢呋喃,二氯甲烷 作为反应溶剂,化学反应 13.09H,反应生成 安曲非宁
参考文献:使用有机叠氮化物进行铁介导的有机锌卤化物的亲电子胺化反应.
标题:使用有机叠氮化物进行铁介导的有机锌卤化物的亲电子胺化反应.
摘要:各种烷基,芳基和杂芳基锌卤化物都被高度官能化的烷基,芳基和杂环叠氮化物胺化.反应在fecl3(0.5当量)存在下于50oc的条件下在1小时内平稳进行,从而以高收率提供了相应的仲胺.该方法扩展到了肽叠氮化物,并为芳构化底物提供了完全保留的构型.为了证明该反应的实用性,我们使用该铁介导的亲电子胺化反应为关键步骤,制备了两种具有药物相关性的胺衍生物.
DOI:10.1002/anie.201911704

专利信息

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:US-4412075-A
优先权日:1981-01-16
标题 :Process for the preparation of quinolin-4-ones
发明人：BAUDOUIN MICHEL; DESBOIS MICHEL
权利人:RHONE POULENC SANTE
摘要:1,2,3,4-Tetrahydroquinolin-4-ones of the formula: ##STR1## wherein R represents a hydrogen or halogen atom, an alkyl radical (1 to 4 carbon atoms), an alkoxy radical (1 to 4 carbon atoms) or the trifluoromethyl radical, and R 1 represents a hydrogen atom, an alkyl radical (1 to 4 carbon atoms) or the trifluoromethyl radical, are prepared by cyclizing a 3-anilinopropionic acid of the formula: ##STR2## (wherein R and R 1 are as hereinbefore defined) in a mixture of hydrofluoric acid and boron trifluoride. n The quinolinone products are useful intermediates in the synthesis of therapeutically active substances.

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:US-4778805-A
优先权日:1987-06-18
标题:4,7-benzofurandione derivatives useful as inhibitors of leukotriene synthesis
发明人：ADAMS JULIAN; GUINDON YVAN; BELANGER PATRICE C; BELLEY MICHEL L; ROKACH JOSHUA
权利人:MERCK FROSST CANADA
摘要:4,7-Benzofurandione derivatives of Formula I, pharmaceutical compositions, and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents. Also disclosed are novel intermediates useful for the preparation of the 4,7-benzofurandiones of this invention. ##STR1##

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