An efficient reverse Diels-Alder approach for the synthesis of N-alkyl bismaleimides
Bismaleimides are useful precursors for Diels-Alder reactions, Michael additions, and thiol-maleimide based conjugation for the synthesis of materials and polymers. Use of bismaleimide cross linkers for generating polymers, bioconjugate molecules, and useful imaging molecules is an active area of research. An efficient and practical synthetic protocol for N-alkyl bis-maleimide cross linkers starting from furan protected maleimide employing a reverse Diels-Alder reaction is reported.
Rao, Venkataramanarao,Navath, Suryakiran,Kottur, Mohankumar,McElhanon, James R.,McGrath, Dominic V.
p. 5011 - 5013
(2013/09/02)
A two-directional strategy for the diversity-oriented synthesis of macrocyclic scaffolds
Macrocyclic compounds represent a structural class with exceptional potential for biological activity; however, they have historically been underrepresented in screening collections and synthetic libraries. In this article we report the development of a highly step-efficient strategy for the diversity-oriented synthesis of complex macrocyclic architectures, using a modular approach based on the two-directional synthesis of bifunctional linear precursors and their subsequent combination in a two-directional macrocyclisation process. In this proof of principle study, the synthesis of 14 such compounds was achieved. Cheminformatic analysis of the compounds produced suggests that they reside in biologically relevant regions of chemical space and the compounds were screened for activity against two cancer cell lines.
O'Connell, Kieron M. G.,Beckmann, Henning S. G.,Laraia, Luca,Horsley, Helen T.,Bender, Andreas,Venkitaraman, Ashok R.,Spring, David R.
supporting information
p. 7545 - 7551
(2012/10/29)
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