161958-61-8Relevant articles and documents
PYRROLIDINE DERIVATIVES AS INHIBITOR OF FIBROBLAST ACTIVATION PROTEIN (FAP) AND PHARMACEUTICAL COMPOSITION INCLUDING THE SAME
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Paragraph 3508; 3512-3514, (2020/11/24)
The FAP inhibitor is represented by the following formula X. The present invention relates to a pyrrolidine derivative or a pharmaceutically acceptable salt thereof. Chem. X.
Proton pump inhibitors
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Paragraph 0176, (2015/11/16)
A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R 1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R 2 , R 3 and R 4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R 5 and R 6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.
Development of a gold-multifaceted catalysis approach to the synthesis of highly substituted pyrroles: Mechanistic insights via Huisgen cycloaddition studies
Ngwerume, Simbarashe,Lewis, William,Camp, Jason E.
, p. 920 - 934 (2013/04/10)
A novel gold-catalyzed method for the regioselective synthesis of highly substituted pyrroles directly from oximes and alkynes was developed via independent optimization of two key steps of the process. Importantly, a cationic gold(I) species was shown to activate multiple steps along the reaction pathway and therefore act as a multifaceted catalyst. Initial gold-promoted addition of the oxime oxygen to the activated alkyne afforded the O-vinyloxime in situ. The O-vinyloxime was subsequently transformed into the pyrrole via a gold-catalyzed tautomerization, [3,3]-sigmatropic rearrangement, and cyclodehydration process. Notably, this method provides a functional group handle in the form of an ester at the 3/4-position for further exploitation. The proposed mechanistic pathway is supported by a novel application of the Huisgen cycloaddition click reaction, which was used to probe the relative stability of substituted O-vinyloximes. The intermediacy of N-alkenylhydroxylamine O-vinyl ethers and imino ketones or imino aldehydes along the reaction pathway were determined by high-temperature 1H, 2H{1H}, and 13C{1H} NMR experiments. X-ray crystallographic evidence was used to further support the mechanistic hypothesis.
