Frontispiece: Modular Bi‐Directional One‐Pot Strategies for the Diastereoselective Synthesis of Structurally Diverse Collections of Constrained β‐Carboline‐Benzoxazepines. Issue 57 (12th October 2017)

• Record Type: Journal Article
• Authors: Srinivasulu, Vunnam; Mazitschek, Ralph; Kariem, Noor M.; Reddy, Amarnath; Rabeh, Wael M.; Li, Liang; O'Connor, Matthew John; Al‐Tel, Taleb H.
• Is Part Of: Chemistry. Volume 23:Issue 57(2017)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2017-10-12
• Subjects: aza-Michael addition -- benzoxazepines -- diversity oriented synthesis. -- Pictet–Spengler reaction -- stereoselective synthesis; Chemistry -- Periodicals; 540
• DOI: 10.1002/chem.201785764
• Languages: English
• ISSNs: 0947-6539

Abstract

Abstract : 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. onpage 14182 ff.