625820-83-9Relevant academic research and scientific papers
Enantioselective synthesis of β-fluoroamines from β-amino alcohols: Application to the synthesis of LY503430
Duthion, Beranger,Pardo, Domingo Gomez,Cossy, Janine
supporting information; experimental part, p. 4620 - 4623 (2010/12/19)
N,N-Dialkyl-β-amino alcohols were enantiospecifically and regioselectively rearranged by using N,N-diethylaminosulfur trifluoride (DAST) to give optically active β-fluoroamines in excellent yields and enantiomeric excesses. This rearrangement was applied to the enantioselective synthesis of LY503430, a potential therapeutic agent for Parkinson's disease.
Diastereomeric salt resolution based synthesis of LY503430, an AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) potentiator
Magnus, Nicholas A.,Aikins, James A.,Cronin, Jason S.,Diseroad, William D.,Hargis, Amy D.,LeTourneau, Michael E.,Parker, Bruce E.,Reutzel-Edens, Susan M.,Schafer, John P.,Staszak, Michael A.,Stephenson, Gregory A.,Tameze, Shella L.,Zollars, Lisa M. H.
, p. 621 - 628 (2012/12/25)
This article describes the development and optimization of chemical reactions and subsequent preparation of the API LY503430 under cGMPs to fund first human dose (FHD) clinical evaluation as a potential therapeutic agent for Parkinson's disease. Reasons and rationale are presented for changes in solvents and reagents. One of the major developments presented here is the replacement of a chiral chromatography with a diastereomeric salt resolution. This article also discusses a preferred orientation issue with LY503430 which complicated the XRPD analysis.
