679392-25-7Relevant academic research and scientific papers
BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
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, (2011/06/16)
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
Practical asymmetric synthesis of a non-peptidic αvβ 3 antagonist
Keen, Stephen P.,Cowden, Cameron J.,Bishop, Brian C.,Brands, Karel M. J.,Davies, Antony J.,Dolling, Ulf H.,Lieberman, David R.,Stewart, Gavin W.
, p. 1771 - 1779 (2007/10/03)
(Chemical Equation Presented) The development of a practical and highly convergent synthesis of an αvβ3 antagonist is described. The two key fragments present in this compound, a tetrahydropyrido[2,3-b]azepine ring system and a chiral 3-aryl-5-oxopentanoic acid, were constructed independently and then coupled at a late stage using a Wittig reaction. The pyridoazepine moiety was prepared from N-Boc 6-chloro-2-aminopyridine via directed ortho-metalation/alkylation followed by in situ cyclization. A Suzuki reaction was then used to attach the propionaldehyde side-chain required for Wittig coupling. The coupling partner was prepared from asymmetric methanolysis of a 3-substituted glutaric anhydride followed by elaboration of the acid moiety to the requisite β-keto phosphorane. Using this route, kilogram quantities of the desired drug candidate were prepared.
