187036-01-7Relevant articles and documents
Cu-Catalyzed Direct Amination of Cyclic Amides via C-OH Bond Activation Using DMF
Chen, Peng,Luo, Kaixiu,Yu, Xianglin,Yuan, Xu,Liu, Xiaoyu,Lin, Jun,Jin, Yi
supporting information, p. 6547 - 6551 (2020/09/02)
Herein, we describe a Cu-catalyzed approach to directly accessing aromatic heterocyclic amines from cyclic amides. The most-reported methods for cyclic amide conversions to aromatic heterocyclic amines use an activating group, such as a halogen atom or a
Traceless linker: Oxidative activation and displacement of a sulfur-based linker
Gayo, Leah M.,Suto, Mark J.
, p. 211 - 214 (2007/10/03)
The construction of small heterocycles using solid-phase chemistry is usually done through the use of a polar group to attach the compounds to the resin. These polar functionalities invariably become part of the structure and eventually limit the structure-activity relationships derived from these compounds. We have identified a method for overcoming some of these limitations. A sulfur-based linker has been identified that can serve not only as a point of attachment for a small heterocycle, but also as a means to introduce further diversity into the molecule. The linker remains inert until 'activated' by oxidation. A limiting amount of a nucleophile can then be used to cleave the molecule from the resin and introduce additional diversity into the molecule.
