427-49-6Relevant articles and documents
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Dobrina,Joffe
, (1977)
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Carry over of impurities: A detailed exemplification for glycopyrrolate (NVA237)
Allmendinger, Thomas,Bixel, Dominique,Clarke, Adrian,Di Geronimo, Laura,Fredy, Jean-Wilfried,Manz, Marco,Gavioli, Elena,Wicky, Regine,Schneider, Martin,Stauffert, Fabien J.,Tibi, Markus,Valentekovic, Darko
, p. 1754 - 1769 (2013/01/15)
The original synthesis of glycopyrrolate (NVA237) was revised and shortened into an essentially one-pot process. Without isolating the intermediates, their purification became obsolete, thereby increasing the possibility of the carry over of impurities. For that reason, the actual, potential, and theoretical impurities of the starting materials cyclopentyl mandelic acid and 1-methyl-pyrrolidin-3-ol as well as byproducts which may occur during the synthesis were thoroughly investigated; furthermore, their transformation to possible impurities in the drug substance along the new synthetic route was performed to exclude them as actual impurities in the drug substance with certainty. The question is raised how detailed such investigation-which are fairly manageable for a simple product like glycopyrrolate-need to be.
Synthesis and optimization of novel and selective muscarinic M3 receptor antagonists
Kumar, Naresh,Kaur, Kirandeep,Aeron, Shelly,Dharmarajan, Sankaranarayanan,Silamkoti, Arun D.V.,Mehta, Anita,Gupta, Suman,Chugh, Anita,Gupta, Jang B.,Salman, Mohammad,Palle, Venkata P.,Cliffe, Ian A.
, p. 5256 - 5260 (2008/02/11)
A series of constrained piperidine analogues were synthesized as novel muscarinic M3 receptor antagonists. Evaluation of these compounds in binding assays revealed that they not only have high affinity for the M3 receptor but also have high selectivity over the M2 receptor.
