55171-61-4Relevant academic research and scientific papers
Synthesis of benzo[c][1,8]phenanthrolin-6-one through cyclization of N-(isoquinol-5-yl)-2-bromo-benzamide derivatives
Prado, Soizic,Michel, Sylvie,Tillequin, Francois,Koch, Michel
, p. 1261 - 1265 (2006)
In the course of our search for compounds with potential antitumor properties we have undertaken the synthesis of benzo[c][1,8]phenanthroline derivatives. Our project required the preparation of 8,9-dimethoxy benzo[c][1,8]phenanthrolin-6-ones. This was fi
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series
Elsayed, Mohamed S. A.,Nielsen, Jeffery J.,Park, Sungtae,Park, Jeongho,Liu, Qingyang,Kim, Chang H.,Pommier, Yves,Agama, Keli,Low, Philip S.,Cushman, Mark
, p. 10440 - 10462 (2018)
The present account describes the discovery and development of a new benzo[c]pyrrolo[2,3-h][1,6]naphthyridin-5-one (BPN) JAK inhibitory chemotype that has produced selective JAK inhibitors. Sequential palladium chemistry was optimized for the rapid access
Phenanthridine Derivative Host Heat Shock Cognate 70 Down-Regulators as Porcine Epidemic Diarrhea Virus Inhibitors
Chen, Duo-Zhi,Fan, Shi-Rui,Yang, Bi-Juan,Yao, Huo-Chun,Wang, Yi-Ting,Cai, Jie-Yun,Jing, Chen-Xu,Pan, Zi-Hao,Luo, Miao,Yuze, Yan-Qiu,Liu, Guang-Jin,Hao, Xiao-Jiang
, p. 1175 - 1184 (2021/05/05)
Porcine epidemic diarrhea virus (PEDV) has become increasingly problematic around the world, not only for its hazards to livestock but also due to the possibility that it is a zoonotic disease. Although vaccine therapy has made some progress toward PEDV c
A versatile approach to 1-oxo-, 1-oxo-3,4-dihydro- and 1,3,4-trioxo isoquinoline alkaloids and first total synthesis of the dimeric 1-oxoisoquinoline alkaloids berbanine and berbidine
Schütz, Ramona,Schmidt, Sandra,Bracher, Franz
, (2020/04/15)
We have worked out a very short approach to 1-oxoisoquinoline alkaloids starting from readily available 2-bromobenzamides utilizing a 2-ethoxyvinylboronate as a C2 building block for introduction of the C-3,C-4 unit of the isoquinoline core. TF
Organocatalyst in Direct C(sp2)-H Arylation of Unactivated Arenes: [1-(2-Hydroxyethyl)-piperazine]-Catalyzed Inter-/Intra-molecular C-H Bond Activation
Yadav, Lalit,Tiwari, Mohit K.,Shyamlal, Bharti Rajesh Kumar,Chaudhary, Sandeep
, p. 8121 - 8141 (2020/07/16)
This article describes the identification of 1-(2-hydroxyethyl)-piperazine as a new, cost-effective, highly efficient organocatalyst, which promotes both inter- A nd intra-molecular direct C(sp2)-H arylations of unactivated arenes in the presence of potassium tert-butoxide. While the inter-molecular C-H arylation of unactivated benzenes with aryl halides (Ar-X; X = I, Br, Cl) toward biaryl syntheses underwent smoothly in the presence of only 10 mol percent organocatalyst, the intra-molecular C-H arylation catalytic system composed of 40 mol percent each of the catalyst and the additive (4-dimethylaminopyridine (DMAP)). The novel catalyst was also able to perform both inter- A nd intra-molecular direct arylations simultaneously in a single pot. The mechanistic studies confirmed the involvement of aryl radical anions and proceeded via a single-electron-transfer (SET) mechanism. The large substrate scope, high functional group tolerance, competition experiments, gram-scale synthesis, and kinetic studies further highlight the importance and versatile nature of the methodology as well as the compatibility of the new catalyst. To the best of our knowledge, this is the first report on any organocatalyst that reported detailed investigations of both inter- A nd intra-molecular direct C(sp2)-H arylations of unactivated arenes in a single representation.
Structurally simple phenanthridine analogues based on nitidine and their antitumor activities
Qin, Shu-Qin,Li, Lian-Chun,Song, Jing-Ru,Li, Hai-Yun,Li, Dian-Peng
, (2019/01/30)
A series of novel structurally simple analogues based on nitidine was designed and synthesized in search of potent anticancer agents. The antitumor activity against human cancer cell lines (HepG2, A549, NCI-H460, and CNE1) was performed by 3-(4,5-dimethyl
Synthesis method and anti-tumor application of nitidine derivative
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Paragraph 0045-0047, (2019/03/11)
The invention discloses a preparation method and application of a nitidine derivative, relates to the technical field of organic synthesis, and in particular to an organic chemical synthesis method ofa natural product compound nitidine derivative. Experim
Synthetic method and anti-tumor application of phenanthridine nitidine derivative
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Paragraph 0015; 0045-0047, (2019/03/06)
The invention belongs to the technical field of organic synthetic chemistry, and relates to the field of nitidine drugs, in particular to a synthetic method and anti-tumor application of a phenanthridine nitidine derivative. Experiments prove that the phe
Utilization of BozPhos as an Effective Ligand in Enantioselective C-H Functionalization of Cyclopropanes: Synthesis of Dihydroisoquinolones and Dihydroquinolones
Mayer, Camilla,Ladd, Carolyn L.,Charette, André B.
supporting information, p. 2639 - 2644 (2019/04/17)
The bisphosphine monoxide (R,R)-BozPhos enables enantioselective C-H functionalization of cyclopropanes in a palladium-catalyzed cyclization. The synthesis of a broad spectrum of dihydroisoquinolones and dihydroquinolones in good yields and high enantiomeric excess was achieved through the use of this hemilabile ligand. Furthermore, the isolation of an intermediary palladium(II)-BozPhos complex after oxidative addition was successful and a second complex provided further insight into bond length and angles through a crystal structure.
JANUS KINASE INHIBITORS AND USES THEREOF
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Paragraph 0140, (2019/05/15)
The invention described herein pertains to selective Janus kinase (JAK) inhibitors and methods of use thereof. Also described are methods for treating diseases involved abnormal JAK/STAT signaling pathway in mammals using the described selective JAK inhib
