73387-60-7Relevant academic research and scientific papers
Novel 2-methyl-6-arylpyridines carrying active pharmacophore 4,5-dihydro 2-pyrazolines: synthesis, antidepressant, and anti-tuberculosis evaluation
Sowmya,Poojary, Boja,Revanasiddappa,Vijayakumar,Nikil,Kumar, Vasantha
, p. 7399 - 7422 (2017)
As part of the effort to develop new hybrid molecules for the treatment of depression and tuberculosis, a new series of novel 6-aryl-2-methyl-3-(5-aryl-4,5-dihydro-1H-pyrazol-3yl)pyridines 5a–l were synthesized. These compounds were screened for in vivo a
Access to α,α-dihaloacetophenones through anodic C[dbnd]C bond cleavage in enaminones
Zhang, Zhenlei,Yang, Jiusi,Wu, Kairui,Yu, Renjie,Bu, Jiping,Huang, Zijun,Li, Shaoke,Ma, Xiantao
supporting information, (2021/12/20)
We have developed a method to synthesize α,α-dihaloketones under electrochemical conditions. In this reaction, the Cl- or Br- is oxidized to Cl2 or Br2 at the anode, which undergoes two-step addition reactions with the N,N-dimethyl enaminone, and finally breaks C[dbnd]C of the N,N-dimethyl enaminone to generate α,α-dihaloketones. The electrosynthesis reaction can be conveniently carried out in an undivided electrolytic cell at room temperature. In addition, various functional groups are compatible with this green protocol which can be applied simultaneously to the gram scale without significantly lower yield.
DDQ-mediated oxidative coupling reaction of N,N-dimethyl enaminones with cycloheptatriene
Cheng, Dongping,Yu, Chenze,Pu, Yueqi,Xu, Xiaoliang
supporting information, (2022/01/23)
An efficient 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)-mediated oxidative coupling reaction of N,N-dimethyl enaminones with cycloheptatriene is developed. It provides a variety of α-alkenylated 1,3-dicarbonyl compounds in moderate to good yields under mild conditions.
Efficient synthesis, structure elucidation, and anti-parasitic activities of novel quinolinyl β–enaminones
Khanikar, Shilpika,Kaping, Shunan,Helissey, Philippe,Joshi, Prince,Shaham, Salique Hassan,Mishra, Shikha,Srivastava, Mrigank,Tripathi, Renu,Vishwakarma, Jai N.
, p. 665 - 678 (2021/05/26)
In the present study, a novel series of side chain-modified quinoline β-enaminones were synthesized in good-to-excellent yields. The structures of all the synthesized compounds have been established with the help of spectral and analytical data and also b
An expedient synthesis of highly functionalized 1,3-dienes by employing cyclopropenes asC4units
Jiang, Chengzhou,Wu, Jiamin,Han, Jiabin,Chen, Kai,Qian, Yang,Zhang, Zhengyu,Jiang, Yaojia
supporting information, p. 5710 - 5713 (2021/06/16)
An efficient method has been described to synthesize dicarbonyl functionalized 1,3-dienes by cleaving the CC bond of enaminones with cyclopropenes in the presence of a rhodium catalyst. The acetate-substituted cyclopropenes are judiciously chosen as standardC4units of 1,3-diene precursors. The reactions are believed to undergo a unique cutting and insertion process, involving a CC bond cleavage of the enaminone and insertion of a newC(sp2) source with the formation of two C-C single bonds. A broad range of substrates can be used to synthesize the corresponding 1,3-dienes under very mild reaction conditions, including low catalyst-loading, ambient temperature, and a neutral reaction solvent.
Synthesis of a new series of pyrazolo[1,5-a]pyrimidines as CDK2 inhibitors and anti-leukemia
Almehmadi, Samar J.,Alsaedi, Amani M.R.,Harras, Marwa F.,Farghaly, Thoraya A.
, (2021/10/26)
Based on the structural study of previously known CDK2 inhibitors, a new series of pyrazolo[1,5-a]pyrimidine derivatives was designed and synthesized. The target compounds were biologically assessed as potent CDK2 inhibitors and promising anti-leukemia hi
One-Pot Synthesis of Symmetrical and Asymmetrical 3-Amino Diynes via Cu(I)-Catalyzed Reaction of Enaminones with Terminal Alkynes
Zhang, Changyuan,Guo, Huosheng,Chen, Lulu,Zhang, Jiantao,Guo, Mengping,Zhu, Xuncheng,Shen, Chan,Li, Zeng
supporting information, p. 8169 - 8173 (2021/11/01)
An economical and efficient protocol for the direct construction of amino skipped diynes through the Cu(I)-catalyzed reaction of enaminones and terminal alkynes has been described. Different kinds of symmetrical and asymmetrical 3-amino diynes could be ob
A new approach for the synthesis of novel naphthoquinone chalcone hybrid compounds
Nguyen, Ha-Thanh,Dang Thi, Tuyet Anh,Hoang Thi, Phuong,Le-Nhat-Thuy, Giang,Nguyen Thi, Quynh Giang,Nguyen Tuan, Anh,Le Thi, Tu Anh,Van Nguyen, Tuyen
supporting information, (2021/08/27)
A facile and efficient synthesis of novel naphthoquinone-based chalcone hybrids (7 and 24) via the microwave-assisted one-pot three-component reactions of 2-substituted-1,4-naphthoquinones, N,N-dimethylformamide dimethyl acetal (DMF-DMA), and acetophenone derivatives has been reported. Whereas the synthesis of hybrids 7 proceeded via a condensation, 1,4-addition, rotation, elimination, and [1,3]-H shift sequence of steps, the synthesis of hybrids 24 were formed through a three-step sequence including condensation, 1,4-addition, and elimination reactions.
Sulfonamide/sulfamate switch with a series of piperazinylureido derivatives: Synthesis, kinetic and in silico evaluation as carbonic anhydrase isoforms I, II, IV, and IX inhibitors
Nocentini, Alessio,Moi, Davide,Deplano, Alessandro,Osman, Sameh M.,AlOthman, Zeid A.,Balboni, Gianfranco,Supuran, Claudiu T.,Onnis, Valentina
, (2019/12/09)
We report here a thorough structure-activity relationship (SAR) with piperazinylureido sulfamates as inhibitors of human (h) carbonic anhydrase (CA, EC 4.2.1.1). A SAR investigation over the structure of reported anti-cancer zinc-binder CAIs such as SLC-0
Synthesis and in-vitro anti-proliferative evaluation of some pyrazolo[1,5-a]pyrimidines as novel larotrectinib analogs
Attia, Mohamed H.,Elrazaz, Eman Z.,El-Emam, Soad Z.,Taher, Azza T.,Abdel-Aziz, Hatem A.,Abouzid, Khaled A.M.
, (2019/12/12)
A series of 2-phenyl-7-(aryl)pyrazolo[1,5-a]pyrimidine-3-carbonitriles 11a–j and 2-phenyl-7-(aryl)pyrazolo[1,5-a]pyrimidine-3,6-dicarbonitriles 16a–c was synthesized by the reaction of 5-amino-3-phenyl-1H-pyrazole-4-carbonitrile (5) with 3-(dimethylamino)
