637739-99-2Relevant academic research and scientific papers
Escaping from Flatland: Substituted Bridged Pyrrolidine Fragments with Inherent Three-Dimensional Character
Bloomfield, Graham,Booker-Milburn, Kevin I.,Cox, Brian,Cox, Philip B.,Elliott, Luke D.,Paumier, Romain,Robertson-Ralph, Michael,Zdorichenko, Victor
, p. 1185 - 1190 (2020)
The pressure to deliver new medicines to the patient continues to grow along with increases in compound failure rate, thus putting the current R&D model at risk. Analysis has shown that increasing the three-dimensionality of potential drug candidates decreases the risk of failure and improves binding selectivity and frequency. For this reason many workers have taken a new look at the power of photochemistry as a means to generate novel sp3 rich scaffolds for use in drug discovery programs. Here we report the design, synthesis, and computational structural analysis of a series of 2,4-methanoprolines having inherent 3D character (PMI and PBF scores) significantly higher than that of the broader AbbVie Rule of 3 (Ro3) collection.
Modification of 1-Substituents in the 2-Azabicyclo[2.1.1]hexane Ring System; Approaches to Potential Nicotinic Acetylcholine Receptor Ligands from 2,4-Methanoproline Derivatives
Malpass, John R.,Patel, Anup B.,Davies, John W.,Fulford, Sarah Y.
, p. 9348 - 9355 (2007/10/03)
Successful nucleophilic substitution at a methylene attached to the bridgehead (1-) position of the 2-azabicyclo[2.1.1]hexane ring system opens the way to construction of novel derivatives having a wider range of functional groups attached to the 1-positi
