28860-19-7Relevant academic research and scientific papers
Structurally Diverse Synthesis of Five-, Six-, and Seven-Membered Benzosultams through Electrochemical Cyclization
Liu, Aiyun,Guo, Tiantian,Zhang, Shuangshuang,Yang, Han,Zhang, Qi,Chai, Yonghai,Zhang, Shengyong
supporting information, p. 6326 - 6331 (2021/08/23)
We have developed a metal- and oxidant-free approach to structurally diverse synthesis of benzosultams from aryl sulfonamides through an electrochemical cyclization. Upon variation of the ortho substituent on aryl sulfonamides, five-, six-, and seven-memb
Time-Resolved EPR Revealed the Formation, Structure, and Reactivity of N -Centered Radicals in an Electrochemical C(sp3)-H Arylation Reaction
Alhumade, Hesham,Gao, Renfei,Huang, Cunlong,Lei, Aiwen,Liu, Yichang,Liu, Zhao,Qi, Xiaotian,Shi, Biyin,Wang, Shengchun
supporting information, p. 20863 - 20872 (2021/12/14)
Electrochemical synthesis has been rapidly developed over the past few years, while a vast majority of the reactions proceed through a radical pathway. Understanding the properties of radical intermediates is crucial in the mechanistic study of electroche
N-alkylation of sulfonamides with alcohols by Tf2O
Yu, Ting Ting,Qi, Lan-Jun,Cui, Dong-Mei,Zhang, Chen,Zhao, Yan
supporting information, p. 610 - 612 (2015/08/04)
N-sulfonylpyrrolidines and N-alkyl sulfonamides were efficiently prepared via alkylation of sulfonamides with 1,4- diols or alcohols by Tf2O. The reaction occurred under mild reaction conditions in moderate to high yields and tolerated aryl and aliphatic sulfonamides.
Synthesis of nitromethyl-substituted oxindole derivatives via a desulfonylation cascade
Niu, Ben,Xie, Ping,Bian, Zhaogang,Zhao, Wannian,Zhang, Min,Zhou, Yang,Feng, Lei,Pittman, Charles U.,Zhou, Aihua
supporting information, p. 635 - 638 (2015/03/14)
A cascade reaction giving nitromethyl-substituted oxindole derivatives was developed. The reaction used NaNO2 as the nitro source and potassium peroxydisulfate as an oxidant. This reaction proceeded via a radical mechanism involving substitution-desulfonlylation-cyclization steps in one pot and afforded good yields under mild conditions without using toxic metal catalysts. The resultant nitromethyl-substituted oxindole derivatives are convenient and valuable structures for different derivative syntheses.
PAR2 RECEPTOR ANTAGONISTS
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Page/Page column 30, (2014/02/16)
Compounds of formula (I) or pharmaceutically acceptable salts, solvates or hydrates thereof wherein P, Q, X, Y, R1, R2, R3, R10, R11, and R12 are as defined in the claims, and the use those compounds in medicine.
RECEPTOR ANTAGONISTS
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Page/Page column 16, (2014/02/16)
N-(4-carbamimidoylphenyl)-amide derivatives having utility in therapy as PAR2 receptor antagonists.
Discovery of novel HCV inhibitors: Synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B
Zhang, Xiaoyan,Zhang, Nanjing,Chen, Guangming,Turpoff, Anthony,Ren, Hongyu,Takasugi, James,Morrill, Christie,Zhu, Jin,Li, Chunshi,Lennox, William,Paget, Steven,Liu, Yalei,Almstead, Neil,George Njoroge,Gu, Zhengxian,Komatsu, Takashi,Clausen, Valerie,Espiritu, Christine,Graci, Jason,Colacino, Joseph,Lahser, Fred,Risher, Nicole,Weetall, Marla,Nomeir, Amin,Karp, Gary M.
, p. 3947 - 3953 (2013/07/27)
A novel series of 6-(indol-2-yl)pyridine-3-sulfonamides was prepared and evaluated for their ability to inhibit HCV RNA replication in the HCV replicon cell culture assay. Preliminary optimization of this series furnished compounds with low nanomolar potency against the HCV genotype 1b replicon. Among these, compound 8c has identified as a potent HCV replicon inhibitor (EC50 = 4 nM) with a selectivity index with respect to cellular GAPDH of more than 2500. Further, compound 8c had a good pharmacokinetic profile in rats with an IV half-life of 6 h and oral bioavailability (F) of 62%. Selection of HCV replicon resistance identified an amino acid substitution in HCV NS4B that confers resistance to these compounds. These compounds hold promise as a new chemotype with anti-HCV activity mediated through an underexploited viral target.
Evidence for an Isocyanate Formation in the Alkaline Hydrolysis of N1-Alkyl Derivatives of Chlorpropamide, Inhibitors of Aldehyde Dehydrogenase
Bergon, M.,Vigroux, A.,Tisnes, P.
, p. 946 - 947 (2007/10/02)
Trapping of a propyl isocyanate intermediate and entropies of activation data are consistent with an elimination-addition mechanism AxhDH + DN (E1cB) for the hydrolysis of 1-alkyl-1--3-n-propylurea, the N1-alkyl derivatives of chlorpropamide, inhibitors of aldehyde dehydrogenase.
