- Synthesis and characterization of novel sulfonamides derivatives and their antimicrobial, antioxidant and cytotoxicity evaluation
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Five novel sulfonamides derivatives HR5-HR8 and HR14 were synthesized by sulfonylation of primary or secondary amine in the presence of base through nucleophilic substitution reaction. Structural elucidation was carried out through FT-IR, UV, 1
- Rehman, Hajira,Qadir, Abdul,Ali, Zulfiqar,Nazir, Shahid,Zahra, Asmat,Shahzady, Tanzeela Gulab
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- Stereospecific Synthesis of cis-2,5-Disubstituted Pyrrolidines via N, O-Acetals Formed by Hydroamination Cyclization-Hydroalkoxylation of Homopropargylic Sulfonamides in HFIP
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We reported a novel two-step stereoselective synthesis of functionalized pyrrolidines from homopropargylic sulfonamides and nucleophiles via an isolable N,O-acetal intermediates. This reaction features mild conditions and good scope of substrates. In addition, the use of hexafluoroisopropanol, acting as a solvent, an additive, a weak nucleophile, and a good leaving group, is pivotal to the success of the method. Moreover, reactions of chiral homopropargylic sulfonamides afford only 2,5-cis-disubstituted pyrrolidines with high diastereoselectivity (up to >99:1 dr) and enantioselectivity (up to >99% ee). The overall reaction constitutes a formal 1,1-bifunctionalization of terminal alkynes, which has hitherto been reported only rarely. Additionally, this method provides efficient access to pharmaceutical intermediate and to carry out postmodification of natural products.
- Cao, Xiaohui,Chang, Weixing,Li, Jing,Liu, Lingyan,Shi, Xiaoyu,Wang, Weilin,Xiao, Weiguo,Zuo, Xiaodan
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p. 7045 - 7059
(2020/07/07)
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- Design, synthesis and biological evaluation of N-phenylsulfonylnicotinamide derivatives as novel antitumor inhibitors
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A series of novel N-phenylsulfonylnicotinamide derivatives (1-24) have been synthesized and evaluated as potential EGFR tyrosine kinase (TK) inhibitors. Among all the compounds, compound 10 (5-bromo-N-(4-chlorophenylsulfonyl) nicotinamide) showed the most
- Zhang, Hui,Lu, Xiang,Zhang, Li-Rong,Liu, Jia-Jia,Yang, Xian-Hui,Wang, Xiao-Ming,Zhu, Hai-Liang
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experimental part
p. 1411 - 1416
(2012/04/23)
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- Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors
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A series of pyridine acyl sulfonamide derivatives (1-24) have been designed and synthesized and their biological activities were also evaluated as potential cyclooxygenase-2 (COX-2) inhibitors. Among all the compounds, compound 23 displayed the most poten
- Lu, Xiang,Zhang, Hui,Li, Xi,Chen, Guo,Li, Qing-Shan,Luo, Yin,Ruan, Ban-Feng,Chen, Xian-Wei,Zhu, Hai-Liang
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experimental part
p. 6827 - 6832
(2012/02/02)
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