1416904-94-3Relevant articles and documents
Chirality-Driven Mode of Binding of α-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS)
Feng, Yuting,Park, Jaeok,Li, Shi-Guang,Boutin, Rebecca,Viereck, Peter,Schilling, Matthew A.,Berghuis, Albert M.,Tsantrizos, Youla S.
, p. 9691 - 9702 (2019)
Thienopyrimidine-based allosteric inhibitors of the human farnesyl pyrophosphate synthase (hFPPS), characterized by a chiral α-aminophosphonic acid moiety, were synthesized as enantiomerically enriched pairs, and their binding mode was investigated by X-ray crystallography. A general consensus in the binding orientation of all (R)- and (S)-enantiomers was revealed. This finding is a prerequisite for establishing a reliable structure-activity relationship (SAR) model.
Chiral α-amino phosphonates via rhodium-catalyzed asymmetric 1,4-addition reactions
Lefevre, Nicolas,Brayer, Jean-Louis,Folleas, Benoiit,Darses, Sylvain
, p. 4274 - 4276 (2013/09/12)
A new approach for the preparation of enantioenriched α-amino phosphonates and derivatives is described. Indeed, the rhodium-catalyzed asymmetric 1,4-addition of potassium organotrifluoroborates to dehydroaminophosphonates afforded α-amino phosphonates in