654084-12-5Relevant academic research and scientific papers
Synthesis of New Annelated Indole Systems : New Entry in the E-azaeburnane series.
Melnyk, Patricia,Legrand, Bruno,Gasche, Jeannette,Ducrot, Pierre,Thal, Claude
, p. 1941 - 1952 (1995)
Starting from a judiciously substituted N-aminoindole, the Heck reaction led to new classes of heterocyclic compounds: the pyridopyridazinoindoles 7 and 8 and the pyridodiazepinoindole 15.From compound 7 the pentacyclic E-azaeburnane 21 was prepared.
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.
Synthesis and properties of novel N,C,N terdentate skeleton based on 1,3-di(pyridin-2-yl)benzene moiety—new tricks for old dogs
Tan, Shuai,Wu, Xiugang,Zheng, Yanqiong,Wang, Yafei
supporting information, p. 1951 - 1954 (2019/09/12)
Utilization of intermolecular Friedel–Crafts and intramolecular condensation reaction, novel 1,3-di(pyridine-2-yl)benzene(N,C,N terdentate) skeleton with electro-withdrawing group in 6' position of pyridyl and a cyclization between 6' position of pyridyl and 6 position of benzyl ring were firstly designed and synthesized. The structures of these novel N,C,N terdentate were confirmed by NMR, MS and X-ray single crystalanalyses. The photophysical properties of these compounds were briefly explored.
Palladium-catalyzed intramolecular C-H arylation of 2-halo-: N -Boc- N -arylbenzamides for the synthesis of N-H phenanthridinones
Hu, Quan-Fang,Gao, Tian-Tao,Shi, Yao-Jie,Lei, Qian,Yu, Luo-Ting
, p. 13879 - 13890 (2018/04/25)
A palladium catalyzed synthesis of N-H phenanthridinones was developed via C-H arylation. The protocol gives phenanthridinones regioselectively by one-pot reaction without deprotection. It exhibits broad substrate scope and affords targets in up to 95% yields. Importantly, it could be applied for the less reactive o-chlorobenzamides.
Copper-Catalyzed Cascade Synthesis of [1,2,4]-Triazoloquinazolinones
Lou, Zhenbang,Man, Ningning,Yang, Haijun,Zhu, Changjin,Fu, Hua
supporting information, p. 1395 - 1399 (2018/05/03)
An efficient and practical method for the synthesis of 1,2,4-triazolo[5,1- b ]quinazolin-9(3 H)-ones has been developed via the copper-catalyzed domino reactions of readily available substituted N ′-acetyl-2-bromobenzohydrazides with cyanamide. The protocol uses inexpensive CuI as the catalyst, and no other ligand or additive was required. The target products were prepared in good to excellent yields with tolerance of various functional groups.
A containing iridium metal complex and its organic light-emitting device (by machine translation)
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Paragraph 0066-0069, (2019/01/06)
The present invention provides a containing iridium metal complex and its organic light-emitting device, containing iridium metal complex of the formula (I) as shown in the structure, the structure comprises a 1st ligand and auxiliary ligand, wherein the auxiliary ligand rich electronic in the structure of the double-nitrogen coordination structure will help to stabilize the central trivalent metal cation, while at the same time, will also affect the electron cloud of the distribution of the metal in iridium, and then the whole complex molecular photoelectric nature greatly influenced the, and the double nitrogen coordination structure ligand and the metal of a four-membered ring has stronger rigid, help to reduce unnecessary vibration energy loss, to realize high-efficient light-emitting performance. By adjusting the substituted group and, so that the complex has better thermal stability and chemical properties. The iridium metal complex preparation generator part, in particular as a doping material, device exhibits a low driving voltage, advantages of high luminous efficiency, superior to the existing common OLED device. (by machine translation)
Preparation method and application of pyrazolo[3, 4-b]pyridine compound intermediate
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Paragraph 0087; 0088; 0089, (2016/10/17)
The invention provides a preparation method and application of a pyrazolo[3, 4-b]pyridine compound intermediate. Specifically, the intermediate structure is shown as formula IV, wherein the groups are defined as the specification and claims. The intermedi
ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
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Paragraph 0189; 0192, (2016/10/10)
A compound having a structure of Formula M(LA)x(LB)y(LC)z, where ligand LA is ligand LB is and ligand LC is is disclosed. In Formula M(LA)x(LB)y(LC)z, M is a metal having an atomic number greater than 40; x is 1, 2, or 3; y and z are 0, 1, or 2; x+y+z is the oxidation state of metal M; Z1-Z6 are each C or N; ZD is N or a carbene carbon; rings C and D are independently a 5 or 6-membered carbocyclic or heterocyclic ring; R4 is substituted, while each of R1, R2, R3, RC, RD, R11, R12, and R13 are selected from hydrogen and a variety of moieties; and any adjacent substituents of R1, R2, R3, R4, RC, RD, R11, R12, and R13 are optionally joined to form a ring. Formulations and devices, such as an OLEDs, that include the compound of formula M(LA)x(LB)y(LC)z are also described.COPYRIGHT KIPO 2015
Discovery and SAR of 5-(3-Chlorophenylamino)benzo[ c ][2,6]naphthyridine-8- carboxylic Acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the Treatment of Cancer
Pierre, Fabrice,Chua, Peter C.,Obrien, Sean E.,Siddiqui-Jain, Adam,Bourbon, Pauline,Haddach, Mustapha,Michaux, Jerome,Nagasawa, Johnny,Schwaebe, Michael K.,Stefan, Eric,Vialettes, Anne,Whitten, Jeffrey P.,Chen, Ta Kung,Darjania, Levan,Stansfield, Ryan,Anderes, Kenna,Bliesath, Josh,Drygin, Denis,Ho, Caroline,Omori, May,Proffitt, Chris,Streiner, Nicole,Trent, Katy,Rice, William G.,Ryckman, David M.
experimental part, p. 635 - 654 (2011/03/21)
Herein we chronicle the discovery of CX-4945 (25n), a first-in-class, orally bioavailable ATP-competitive inhibitor of protein kinase CK2 in clinical trials for cancer. CK2 has long been considered a prime cancer drug target because of the roles of deregulated and overexpressed CK2 in cancer-promoting prosurvival and antiapoptotic pathways. These biological properties as well as the suitability of CK2s small ATP binding site for the design of selective inhibitors, led us to fashion novel therapeutic agents for cancer. The optimization leading to 25n (Ki = 0.38 nM) was guided by molecular modeling, suggesting a strong binding of 25n resulting from a combination of hydrophobic interactions, an ionic bridge with Lys68, and hydrogen bonding with the hinge region. 25n was found to be highly selective, orally bioavailable across species (20-51%) and efficacious in xenograft models. The discovery of 25n will allow the therapeutic targeting of CK2 in humans for the first time.
