849928-35-4Relevant academic research and scientific papers
A Robust, Recyclable Resin for Decagram Scale Resolution of (±)-Mefloquine and Other Chiral N-Heterocycles
Kreituss, Imants,Chen, Kuang-Yen,Eitel, Simon H.,Adam, Jean-Michel,Wuitschik, Georg,Fettes, Alec,Bode, Jeffrey W.
supporting information, p. 1553 - 1556 (2016/02/12)
Decagram quantities of enantiopure (+)-mefloquine have been produced via kinetic resolution of racemic mefloquine using a ROMP-gel supported chiral acyl hydroxamic acid resolving agent. The requisite monomer was prepared in a few synthetic steps without chromatography and polymerization was safely performed on a >30 gram scale under ambient conditions. The reagent was readily regenerated and reused multiple times for the resolution of 150 grams of (±)-mefloquine and other chiral N-heterocylces.
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious γ-Secretase Inhibitors
Ye, Xiaocong M.,Konradi, Andrei W.,Smith, Jenifer,Xu, Ying-Zi,Dressen, Darren,Garofalo, Albert W.,Marugg, Jennifer,Sham, Hing L.,Truong, Anh P.,Jagodzinski, Jacek,Pleiss, Michael,Zhang, Hongbin,Goldbach, Erich,Sauer, John-Michael,Brigham, Elizabeth,Bova, Michael,Basi, Guriqbal S.
scheme or table, p. 2195 - 2199 (2010/07/05)
Discovery of a series of pyrazolopiperidine sulfonamide based γ-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold were achieved and this potency increase translated in an improved in vivo efficacy.
