Synthesis of novel and conformationally constrained bridged amino acids as compact modules for drug discovery. Issue 5 (3rd February 2016)

• Record Type: Journal Article
• Authors: Wu, Guolong; Kou, Buyu; Tang, Guozhi; Zhu, Wei; Shen, Hong C.; Liu, Haixia; Hu, Taishan
• Is Part Of: Tetrahedron letters. Volume 57:Issue 5(2016)
• Page Start: 599
• Page End: 602
• Publication Date: 2016-02-03
• Subjects: Amino acid -- Bridged building block -- Compact module -- Conformationally constrained; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tetlet.2015.12.097
• Languages: English
• ISSNs: 0040-4039

Abstract

Graphical abstract: Abstract: As novel scaffolds with rigid inherent three-dimensional conformation, the bridged amino acid building blocks containing both morpholine and pyrrolidine motifs, 2-oxa-5-azabicyclo[2.2.1]heptane-4-carboxylic acid1 and 3-oxa-8-azabicyclo[3.2.1]octane-5-carboxylic acid2, were first synthesized as compact modules for future applications in the optimization of physicochemical and pharmacokinetic properties of drug candidates in drug discovery.