Synthesis of Constrained Benzoxazepines and Imidazopyrazines

Sequencing Groebke–Blackburn–Bienaymé and Aza-Michael Addition Reactions: A Modular Strategy for Accessing a Diverse Collection of Constrained Benzoxazepine and Imidazopyrazine Systems: Vunnam Srinivasulu, Farah Al-Marzooq, Mohamad Hamad, Monther A. Khanfar, Mani Ramanathan, Nelson C. Soares and Taleb H. Al-Tel

Synthesis 2021, 53, DOI: 10.1055/s-0040-1706006


Multicomponent reactions (MCRs) represent an invaluable tool for accessing complex structural frameworks in a straightforward and one-pot manner, often enabling access to a broad diversity of molecules, which can be instrumental for drug discovery campaigns. Recently, the group of Professor Taleb H. Al-Tel from the University of Sharjah (UAE) reported a novel application of MCRs – combining a sequence of Groebke–Blackburn–Bienaymé and aza-Michael addition aractions – which allowed a straightforward one-pot synthesis of a range of interesting heterocyclic structures, including benzoxazepinium scaffolds fused to imidazopyridine and imidazothiazole rings.

Professor Al-Tel said: „A modular and ideal one-pot starting material-based approach for accessing a unique library of polycyclic benzoxazepines with a broad distribution of molecular shapes is reported.”

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