189136-13-8Relevant academic research and scientific papers
COMPOUNDS, COMPOSITIONS AND METHODS FOR STABILIZING TRANSTHYRETIN AND INHIBITING TRANSTHYRETIN MISFOLDING
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, (2021/08/06)
Provided herein are compounds having activity against TTR related conditions, and pharmaceutically accepted salts and solvates thereof. Also provided are methods of using the compounds for inhibiting and preventing TTR aggregation and/or amyloid formation in the peripheral nerves, kidney, cardiac tissue, eye and CNS, and of treating a subject with peripheral TTR amyloidosis.
Synthesis of 5-amino- and 5-hydroxy-3,3-difluoropiperidines
Surmont, Riccardo,Verniest, Guido,Thuring, Jan Willem,Ten Holte, Peter,Deroose, Frederik,De Kimpe, Norbert
supporting information; experimental part, p. 4514 - 4517 (2010/11/18)
Synthetic routes toward new 5-amino- and 5-hydroxy-3,3-difluoropiperidines, which are of high interest as building blocks in medicinal chemistry, are described. The key step involves the N-halosuccinimide-induced cyclization of 2,2-difluoro-4-pentenylamines toward 5-halo-3,3-difluoropiperidines, which were used to synthesize 5-amino-3,3-difluoropiperidine. In a second strategy, iodolactonization of 2,2-difluoro-4-pentenoic acid gave the corresponding ??-lactone, which was transformed into 5-hydroxy-3,3-difluoropiperidine.
