221101-01-5Relevant academic research and scientific papers
Click inspired novel pyrazole-triazole-persulfonimide & pyrazole-triazole-aryl derivatives; Design, synthesis, DPP-4 inhibitor with potential anti-diabetic agents
Nidhar, Manisha,Khanam, Shaziya,Sonker, Priyanka,Gupta, Priya,Mahapatra, Archisman,Patil, Swaraj,Yadav, Brijesh Kumar,Singh, Rahul Kumar,Kumar Tewari, Ashish
supporting information, (2022/01/22)
This work presented the first report on designing, synthesizing of novel pyrazole-triazole-persulfonimide (7a-i) and pyrazole-triazole-aryl derivatives (8a-j) via click reaction using CuI catalyst and evaluated for their anti-diabetic activity and DPP-4 i
Fluorocyclization of Allyl Alcohols and Amines to Access 3-Functionalized Oxetanes and Azetidines
Cao, Shanshan,Li, Linxuan,Liu, Zhaohong,Ning, Yongquan,Wu, Yong,Zanoni, Giuseppe,Zhang, Qi,Zhang, Xinyu
supporting information, p. 3674 - 3679 (2021/05/31)
An efficient method to prepare 3-functionalized oxetanes and azetidines has been realized by fluorocyclization of readily available 2-azidoallyl/2-alkoxyallyl alcohols and amines. Notably, this is the first example applying the fluorocyclization strategy to construct four-membered heterocycles. The pendant electron-donating group (-N3 or -OR) plays a crucial role in polarizing the C= C double bond and facilitating the cyclization process, as verified by DFT and experimental studies.
Ruthenium Carbene-Mediated Construction of Strained Allenes via the Enyne Cross-Metathesis/Cyclopropanation of 1,6-Enynes
Gao, Ming,Gao, Qiangqiang,Hao, Xiangbin,Wu, Ying,Zhang, Qingmin,Liu, Guohua,Liu, Rui
supporting information, p. 1139 - 1143 (2020/02/15)
Herein, we report on the unprecedented dimerization of 1,6-enynes using a commercially available ruthenium complex RuCl2(PPh3)3, which results in a series of bicyclo[3.1.0]hexyl allene derivatives in moderate to excellent yields. Mechanistic investigation indicates that the in-situ-generated ruthenium vinylidene undergoes a site-selective metathesis process to provide allenyl ruthenium carbene, which can be intramolecularly trapped by the pendent C=C bond of enyne through a [2 + 2] cycloaddition/metal elimination process.
Orthogonal Syntheses of 3.2.0 Bicycles from Enallenes Promoted by Visible Light
Serafino, Andrea,Balestri, Davide,Marchiò, Luciano,Malacria, Max,Derat, Etienne,Maestri, Giovanni
supporting information, p. 6354 - 6359 (2020/09/02)
Enallenes can be readily converted into two families of 3.2.0 (hetero)bicycles with high diastereoselectivities through the combination of visible light with a suitable Ir(III) complex (1 mol percent). Two complementary pathways, namely, a photocycloaddit
Structure optimization and bioactivity evaluation of ThDP analogs targeting cyanobacterial pyruvate dehydrogenase E1
Feng, Jiangtao,He, Haifeng,Zhou, Yuan,Cai, Meng,Peng, Hao,Liu, Honglin,Liu, Lei,Feng, Lingling,He, Hongwu
, (2019/11/14)
Harmful cyanobacteria bloom (HCB) has occurred frequently in recent years and it is urgent to develop novel algicides to deal with this problem. In this paper, a series of novel thiamin diphosphate (ThDP) analogs 5a?5g were designed and synthesized target
BETA-LACTAMASE INHIBITORS
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Paragraph 0444; 0448, (2017/04/08)
Described herein are compounds and compositions that modulate the activity of beta -lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
Synthesis, in?vitro anticancer and antibacterial activities and in silico studies of new 4-substituted 1,2,3-triazole–coumarin hybrids
Kraljevi?, Tatjana Gazivoda,Harej, Anja,Sedi?, Mirela,Paveli?, Sandra Kraljevi?,Stepani?, Vi?nja,Drenjan?evi?, Domagoj,Talapko, Jasminka,Rai?-Mali?, Silvana
, p. 794 - 808 (2016/09/23)
The 4-substituted 1,2,3-triazole core in designed coumarin hybrids (4–35) with diverse physicochemical properties was introduced by eco-friendly copper(I)-catalyzed Huisgen 1,3-dipolar cycloaddition under microwave irradiation. Coumarin–1,2,3-triazole–ben
Design, synthesis, biological evaluation and molecular docking of amide and sulfamide derivatives as Escherichia coli pyruvate dehydrogenase complex E1 inhibitors
He, Haifeng,Feng, Jiangtao,He, Junbo,Xia, Qin,Ren, Yanliang,Wang, Fang,Peng, Hao,He, Hongwu,Feng, Lingling
, p. 4310 - 4320 (2016/01/29)
In this study, a series of novel amide derivatives and sulfamide derivatives as potential E. coli PDHc E1 inhibitors were designed and synthesized by optimizing the linker between triazole and benzene ring moieties based on the structure of lead compound
P-TsOH Promoted Au(I)-Catalyzed Consecutive Endo Cyclization of Yne-Tethered Ynamide: Access to Benzofused Dihydroisoquinolones
Nayak, Sanatan,Ghosh, Nayan,Prabagar,Sahoo, Akhila K.
supporting information, p. 5662 - 5665 (2015/12/01)
A novel synthetic route to benzo[f]dihydroisoquinolone through a p-TsOH promoted cascade cyclization of easily accessible diyne-tethered ynamides in the presence of a Au(I)-catalyst is described. This reaction unveils a broad substrate scope, constructing a wide range of benzo[f]dihydroisoquinolones in good yields. The diyne-tethered ynamides are synthesized from inexpensive o-iodoaniline through Sonogashira couplings and the Cu-mediated C-N bond formation. The role of p-TsOH is examined, and the reaction pathway is also deduced. The benzo[f]isoquinoline scaffold is constructed from benzo[f]dihydroisoquinolones.
Metal-free reductive cyclization and isomerization of sulfanyl-1,6-diynes using sodium borohydride
Ito, Yukiteru,Yoshimatsu, Mitsuhiro
supporting information, p. 1758 - 1760 (2015/02/19)
In this study, we demonstrated the metal-free reductive cyclization of sulfanyl-1,6-diynes with sodium borohydride in ethanol in the presence of diazabicyclo[5.4.0]undec-7-ene. 1,6-Diynes 1 and 5a-5h bearing hydrogen or phenyl as the R2 group a
