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1. 发明申请

WO2015112014A1 PROCESS FOR THE CYCLOADDITION OF A HETERO(ARYL) 1,3-DIPOLE COMPOUND WITH A (HETERO)CYCLOALKYNE 审中-公开
标题翻译：环己酮（ARYL）1,3-二烯化合物与（环己基）环烷酮的环化方法
公开(公告)号：WO2015112014A1
公开(公告)日：2015-07-30
申请号：PCT/NL2015/050045
申请日：2015-01-26
申请人： STICHTING KATHOLIEKE UNIVERSITEIT
发明人： VAN DELFT, Floris Louis , DOMMERHOLT, Frederik Jan
IPC分类号： C07D225/02 , C07D225/08 , C07D231/54 , C07D249/16 , C07D261/20 , C07H19/10 , A61K47/48
CPC分类号： C07D487/04 , A61K47/48061 , A61K47/48215 , A61K47/48584 , A61K47/545 , A61K47/60 , A61K47/6855 , C07C269/06 , C07C271/18 , C07C2602/22 , C07C2603/50 , C07D225/02 , C07D225/08 , C07D231/54 , C07D249/16 , C07D261/20 , C07H19/10 , C07K14/473
摘要： The present invention relates to a process comprising the step of reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein: a (hetero)aryl 1,3-dipole compound is defined as a compound comprising a 1,3-dipole functional group, wherein the 1,3-dipole functional group is bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein: (i) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound comprises one or more substituents having a positive value for the para -Hammett substituent constant σ p and/or the meta -Hammett substituent constant σ m , and/or (ii) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound is an electron-poor (hetero)aryl group, wherein an electron-poor (hetero)aryl group is: (ii-a) a (hetero)aryl group wherein the (hetero)aromatic ring system is bearing a positive charge, and/or (ii-b) a (hetero)aryl group wherein the ratio {number of π-electrons present in the (hetero)aromatic ring system} : {number of protons present in the nuclei of the (hetero)aromatic ring system} is lower than 0.167 for a 6-membered ring, or lower than 0.200 for a 5-membered ring; and wherein the (hetero)cycloalkyne is a (hetero)cyclooctyne or a (hetero)cyclononyne according to Formula (1): The invention also relates to the products obtainable by the process according to the invention.
摘要翻译：本发明涉及包括使（杂）芳基-1,3-偶极化合物与（异）环炔反应的步骤的方法，其中：（杂）芳基-1,3-偶极化合物定义为包含 1,3-偶极官能团，其中1,3-偶极官能团与（杂）芳基键合，其中（杂）芳基1,3-偶极化合物是（杂）芳基叠氮化物或（杂）杂）芳基重氮化合物; 其中：（i）（杂）芳基1,3-偶极化合物的（杂）芳基包含一个或多个对位 - 哈米特取代基常数σp和/或间 - 哈米特取代基常数σm具有正值的取代基，（ii）（杂）芳基-1,3-偶极子化合物的（杂）芳基是电子贫（杂）芳基，其中电子贫（杂）芳基是：（ii -a）（杂）芳环体系带有正电荷的（杂）芳基，和/或（ii-b）（杂）芳基，其中存在于（杂）芳环体系}：（杂）芳环体系的核中存在的质子数目对于6元环低于0.167，对于5元环低于0.200; 并且其中（杂）环炔是根据式（1）的（杂）环辛炔或（杂）环壬烯：本发明还涉及通过本发明的方法获得的产物。

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