2567-51-3Relevant articles and documents
Tauroursodeoxycholic acid derivative, and pharmaceutical composition and preparation containing same
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Paragraph 0089-0094, (2021/01/11)
The invention provides a tauroursodeoxycholic acid derivative, a pharmaceutical composition and a preparation containing the tauroursodeoxycholic acid derivative and pharmaceutical application. The tauroursodeoxycholic acid derivative has a structure repr
Palladium-catalyzed olefination of aryl/alkyl halides with trimethylsilyldiazomethane via carbene migratory insertion
Mu, Qiu-Chao,Wang, Xing-Ben,Ye, Fei,Sun, Yu-Li,Bai, Xing-Feng,Chen, Jing,Xia, Chun-Gu,Xu, Li-Wen
supporting information, p. 12994 - 12997 (2018/11/23)
The direct olefination of aryl/alkyl halides with trimethylsilyldiazomethane (TMSD) as a C1- or C2-unit was achieved successfully via a metal carbene migratory insertion process, which offered a new access to afford (E)-vinyl silanes and (E)-silyl-substituted α,β-unsaturated amides in good yields and high chemoselectivity.
Latent Bronsted Base Solvent-Assisted Amide Formation from Amines and Acid Chlorides
Otsuka, Rikuto,Maruhashi, Kazuo,Ohwada, Tomohiko
supporting information, p. 2041 - 2057 (2018/05/04)
Weakly basic amines, including even neutral amines such as nitroaniline and aminocarboxylic acids, react with acid chlorides very efficiently in N, N -dimethylacetamide (DMAC), without addition of a base, to give the corresponding amides in high yields. The role of DMAC and related solvents as latent Bronsted bases was studied in these amidation reactions. Less basic amines, such as aromatic amines, reacted with benzoyl chloride faster than more basic aliphatic amines.
Access to β-lactams by enantioselective palladium(0)-catalyzed C(sp3)-H alkylation
Pedroni, Julia,Boghi, Michele,Saget, Tanguy,Cramer, Nicolai
supporting information, p. 9064 - 9067 (2014/09/17)
β-Lactams are very important structural motifs because of their broad biological activities as well as their propensity to engage in ring-opening reactions. Transition-metal-catalyzed C-H functionalizations have emerged as strategy enabling yet uncommon h
Design, synthesis and evaluation of novel quinazoline-2,4-dione derivatives as chitin synthase inhibitors and antifungal agents
Ji, Qinggang,Yang, Dan,Wang, Xin,Chen, Chunyan,Deng, Qiao,Ge, Zhiqiang,Yuan, Lvjiang,Yang, Xiaolan,Liao, Fei
, p. 3405 - 3413 (2014/06/23)
A series of novel 1-methyl-3-substituted quinazoline-2,4-dione derivatives were designed, synthesized, and characterized by 1H NMR, 13C NMR and MS spectral data. Their inhibition against chitin synthase (CHS) and antifungal activities were evaluated in vitro. Results showed compounds 5b, 5c, 5e, 5f, 5j, 5k, 5l, and 5o had strong inhibitory potency against CHS. Compound 5c, which has the highest potency among these compounds, had a half-inhibition concentration (IC50) of 0.08 mmol/L, while polyoxin B as positive drug had IC50 of 0.18 mmol/L. These IC 50 values of compounds 5i, 5m, 5n, and 5s were greater than 0.75 mmol/L, which revealed that those compounds had weak inhibition activity against CHS. Moreover, most of these compounds exhibited moderate to excellent antifungal activities. In detail, to Candida albicans, the activities of compound 5g and 5k were 8-fold stronger than that of fluconazole and 4-fold stronger than that of polyoxin B; to Aspergillus flavus, the activities of 5g, 5l and 5o were16-fold stronger than that of fluconazole and 8-fold stronger than that of polyoxin B; to Cryptococcus neoformans, the minimum-inhibition- concentration (MIC) values of compounds 5c, 5d, 5e and 5l were comparable to those of fluconazole and polyoxin B. The antifungal activities of these compounds were positively correlated to their IC50 values against CHS. Furthermore, these compounds had negligible actions to bacteria. Therefore, these compounds were promising selective antifungal agents.
Triazoloamides as potent γ-secretase modulators with reduced hERG liability
Fischer, Christian,Zultanski, Susan L.,Zhou, Hua,Methot, Joey L.,Shah, Sanjiv,Nuthall, Hugh,Hughes, Bethany L.,Smotrov, Nadja,Hill, Armetta,Szewczak, Alexander A.,Moxham, Christopher M.,Bays, Nathan,Middleton, Richard E.,Munoz, Benito,Shearman, Mark S.
scheme or table, p. 3140 - 3146 (2012/06/04)
Synthesis and SAR studies of novel aryl triazoles as gamma secretase modulators (GSMs) are presented in this communication. Starting from our aryl triazole leads, optimization studies were continued and the series progressed towards novel amides and lactams. Triazole 57 was identified as the most potent analog in this series, displaying single-digit nanomolar Aβ42 IC 50 in cell-based assays and reduced affinity for the hERG channel.
Improved procedure for the synthesis of enamine N-oxides
Bernier, David,Blake, Alexander J.,Woodward, Simon
, p. 4229 - 4232 (2008/09/20)
(Chemical Equation Presented) An improved procedure for the preparation of enamine N-oxides involving aminolysis of epoxides, chlorination, N-oxidation, and dehydrochlorination is described. Although isolated β-chloroamine N-oxides are prone to rearrangem
AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC CHANNELS
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Page 50, (2010/02/10)
Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents wherein: X is -N- or -CH-; n is from 0 to 3.