763129-62-0Relevant academic research and scientific papers
Tetrazolones as a Carboxylic Acid Bioisosteres
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Paragraph 0263; 0264; 0265; 0266; 0267; 0268; 0269, (2016/08/17)
The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
A one-pot synthesis of tetrazolones from acid chlorides: Understanding functional group compatibility, and application to the late-stage functionalization of marketed drugs
Duncton, Matthew A. J.,Singh, Rajinder
supporting information, p. 9338 - 9342 (2016/10/13)
A one-pot and scalable synthesis of tetrazolones (tetrazol-5-ones) from acid chlorides using azidotrimethylsilane is presented. The reaction tolerates many functional groups and can furnish aryl-, heteroaryl-, alkenyl-, or alkyl-substituted tetrazolone products in moderate to excellent yield (14-94%). No reduction in yield was observed when the reaction was undertaken on a larger-scale (20-36 g). The method could be used for the late-stage functionalization of pharmaceuticals, to provide tetrazolone congeners of the marketed drugs aspirin, indomethacin, probenecid, telmisartan, bexarotene, niacin (vitamin B3), and the active metabolite of the recently-launched immuno-modulatory agent, BG-12 (Tecfidera). The ability of a tetrazolone group to serve as a bioisostere of a carboxylic acid, and to improve drug pharmacokinetic profiles is also highlighted.
INSECTICIDAL PHTHALAMIDE DERIVATIVES
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Page 70, (2008/06/13)
Novel insecticidal phthalamide derivatives of the formula (I), in which is a 5- or 6- membered heterocyclic group, a plurality of processes for preparing these compounds and their use for controlling pests.
Process for the preparation of 1-4-disubstituted-5 (4H)-tetrazolinones
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, (2008/06/13)
1,4-Disubstituted-5(4H)-tetrazolinones of the formula (I) STR1 wherein R1, R2 and R3 have the meanings given in the specification), which are known to be useful as herbicides, can be obtained in very good yields by reacting the corresponding 1-substituted-5(4H)-tetrazolinones with the corresponding carbamoyl chlorides in the presence of 4-dimethylaminopyridine.
