Invention Grant
US08552183B2 Process for the covalent coupling of two molecules by means of a diels-alder reaction with inverse electron requirement
有权
通过具有反电子需求的狄尔斯 - 阿尔德反应共价偶联两个分子的方法
- Patent Title: Process for the covalent coupling of two molecules by means of a diels-alder reaction with inverse electron requirement
- Patent Title (中): 通过具有反电子需求的狄尔斯 - 阿尔德反应共价偶联两个分子的方法
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Application No.: US12304982Application Date: 2007-06-18
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Publication No.: US08552183B2Publication Date: 2013-10-08
- Inventor: Manfred Wiessler , Eduard Müller , Peter Lorenz , Christian Kliem , Heinz Fleischhacker
- Applicant: Manfred Wiessler , Eduard Müller , Peter Lorenz , Christian Kliem , Heinz Fleischhacker
- Applicant Address: DE Heidelberg
- Assignee: Deutsches Krebsforschungszentrum Stiftung des Offentlichen Rechts
- Current Assignee: Deutsches Krebsforschungszentrum Stiftung des Offentlichen Rechts
- Current Assignee Address: DE Heidelberg
- Agency: Perkins Coie LLP
- Agent Viola T. Kung
- Priority: EP06012414 20060616
- International Application: PCT/EP2007/005361 WO 20070618
- International Announcement: WO2007/144200 WO 20071221
- Main IPC: C07D221/22
- IPC: C07D221/22 ; C07D237/26 ; C07D491/04 ; C07D491/08

Abstract:
The present invention relates to a process for linking two molecules by means of a Diels Alder reaction with inverse electron requirement (DARinv), comprising the following steps: reaction of a (a) triazine or tetrazine with one or more electron-attracting substituents on the ring as a diene component, the electron-attracting substituents being selected from: COOR C(O)NR2 CX3 (X=halogen) halogen CN SO2—R or SO3—R PR2 wherein R═H, alkyl, aryl, heterocycle, which in turn may be substituted, where appropriate, with alkyl, OH, SH, halogen, aryl, heterocycle, nitro, carboxyamido or amine group. —heterocyclic rings having 1, 2 or 3 N, O or S atoms with a ring size of 5 or 6 ring members, which are substituted with at least one carboxyl, sulfonic acid or phosphone group with (b) an isolated double bond or triple bond in a (hetero)carbocyclic ring or an isolated olefinic double bond or triple bond in a linear or branched hydrocarbon chain which may also contain heteroatoms, where appropriate, as a dienophile component.
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