Chemistry - A European Journal
Chemistry - A European Journal
5 years ago

Frontispiece: Modular Bi-Directional One-Pot Strategies for the Diastereoselective Synthesis of Structurally Diverse Collections of Constrained β-Carboline-Benzoxazepines

Frontispiece: Modular Bi-Directional One-Pot Strategies for the Diastereoselective Synthesis of Structurally Diverse Collections of Constrained β-Carboline-Benzoxazepines
Amarnath Reddy, Noor M. Kariem, Vunnam Srinivasulu, Wael M. Rabeh, Liang Li, Ralph Mazitschek, Taleb H. Al-Tel, Matthew John O'Connor
Modular access to a range of tailored heterocyclic scaffolds with diverse 3D-complexity is provided by a novel cascade one-pot methodology based on Pictet–Spengler/aza-Michael addition and Schiff base/aza-Michael addition/reduction protocols. The versatile approach is highly diastereoselectivity and provides direct access to drug-like molecules in good yields. The large substrate scope will enable broad coverage of chemical space and allow for rapid SAR exploration. For more information see the Full Paper by R. Mazitschek, T. H. Al-Tel, et al. on page 14182 ff.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/chem.201785764

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