869725-53-1Relevant articles and documents
Construction of 2-Arylbenzo[4,5]thieno[2,3-d]thiazole Skeleton via CuCl/S-Mediated Three-Component Reaction
Zhang, Wei,Tao, Shanqing,Ge, Huaibin,Li, Qiao,Ai, Zhenkang,Li, Xiaoxian,Zhang, Beibei,Sun, Fengxia,Xu, Xiaqing,Du, Yunfei
supporting information, p. 448 - 452 (2020/02/04)
An exclusive thiophene-fused polycyclic I-conjugated 2-arylbenzo[4,5]thieno[2,3-d]thiazole skeleton was constructed via a one-pot CuCl-mediated three-component reaction, using 2-(2-bromophenyl)acetonitrile and aromatic aldehydes as substrates and elementa
tBuOK-Promoted Cyclization of Imines with Aryl Halides
Li, Ya-Wei,Zheng, Hong-Xing,Yang, Bo,Shan, Xiang-Huan,Qu, Jian-Ping,Kang, Yan-Biao
supporting information, p. 4553 - 4556 (2020/06/08)
A transition-metal-free indole synthesis using radical coupling of 2-halotoluenes and imines via the later-stage C-N bond construction was reported for the first time. It includes an aminyl radical generation by C-H cleaving addition of 2-halotoluenes to imines via the carbanion radical relay and an intramolecular coupling of aryl halides with aminyl radicals. One standard condition can be used for all halides including F, Cl, Br, and I. No extra oxidant or transition metal is required.
Strategy for Overcoming Full Reversibility of Intermolecular Radical Addition to Aldehydes: Tandem C-H and C-O Bonds Cleaving Cyclization of (Phenoxymethyl)arenes with Carbonyls to Benzofurans
Zheng, Hong-Xing,Shan, Xiang-Huan,Qu, Jian-Ping,Kang, Yan-Biao
supporting information, p. 3310 - 3313 (2018/06/11)
An intermolecular addition of carbon radicals enabled by a cascade radical coupling strategy is developed. It includes an intermolecular alkyl radical addition to a carbonyl group followed by an intramolecular alkoxy radical addition to haloarenes and produces substituted benzofurans in high yields. The radical nature of this reaction is explored by radical trapping experiments and EPR analysis. The mechanism is investigated by KIE experiments and control experiments. This method could provide rapid and practical access to the key intermediate of TAM-16, a safe and potent antibacterial agent for treating tuberculosis, and, therefore, is of great importance for organic synthesis and the pharmaceutical industry.
An efficient synthesis of 4-isochromanones via Parham-type cyclization with Weinreb amide
Wang, Chaolei,Wu, Zheng,Wang, Jia,Liu, Jie,Yao, Hequan,Lin, Aijun,Xu, Jinyi
, p. 8172 - 8177 (2015/12/30)
The synthesis of 4-isochromanones via Parham-type cyclization with Weinreb amide as the internal electrophilic group, t-BuLi as the lithium reagent was described. The reaction was efficient and could be completed in one minute. The application scope of this new protocol was investigated and the desired products could be obtained in good to excellent yields. Besides, the synthetic potential of this method was further demonstrated by the synthesis of natural product (±)-XJP, which was obtained in six steps with overall yield up to 54%.
Intermolecular domino reaction of two Aryl iodides involving two C-H functionalizations
Sickert, Marcel,Weinstabl, Harald,Peters, Brendan,Hou, Xiao,Lautens, Mark
supporting information, p. 5147 - 5151 (2014/05/20)
A palladium-catalyzed intermolecular cross-coupling of two aryl iodides is reported, giving polycyclic ring systems with a high level of convergence and efficiency. Pendulum Reaction: 1 Pd complex catalyzes the intermolecular reaction of 2 aryl iodides to
Discovery of INCB9471, a potent, selective, and orally bioavailable CCR5 antagonist with potent anti-HIV-1 activity
Xue, Chu-Biao,Chen, Lihua,Cao, Ganfeng,Zhang, Ke,Wang, Anlai,Meloni, David,Glenn, Joseph,Anand, Rajan,Xia, Michael,Kong, Ling,Huang, Taisheng,Feng, Hao,Zheng, Changsheng,Li, Mei,Galya, Laurine,Zhou, Jiacheng,Shin, Niu,Baribaud, Fredric,Solomon, Kim,Scherle, Peggy,Zhao, Bitao,Diamond, Sharon,Emm, Tom,Keller, Douglas,Contel, Nancy,Yeleswaram, Swamy,Vaddi, Kris,Hollis, Gregory,Newton, Robert,Friedman, Steven,Metcalf, Brian
scheme or table, p. 483 - 487 (2011/03/20)
To identify a CCR5 antagonist as an HIV-1 entry inhibitor, we designed a novel series of indane derivatives based on conformational considerations. Modification on the indane ring led to the discovery of compound 22a (INCB9471) that exhibited high affinit
Dibenzyl Amine Compounds and Derivatives
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Page/Page column 33, (2010/11/28)
Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid le
Dibenzyl Amine Compounds and Derivatives
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Page/Page column 37, (2010/11/28)
Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
Synthesis of benzylisoquinoline derivatives possessing electron-withdrawing substituents on the benzene ring of the isoquinoline skeleton
Severin, René,Mujahidin, Didin,Reimer, Jessica,Doye, Sven
, p. 683 - 700 (2008/09/18)
3,4-Dihydrobenzylisoquinolines and 1,2,3,4-tetrahydrobenzyl-isoquinolines possessing electron withdrawing substituents on the benzene ring of the isoquinoline framework are easily accessible by a synthetic approach that takes advantage of a Sonogashira coupling to build up the C1-C8a bond of the isoquinoline skeleton and a Ti-catalyzed intramolecular hydroamination of an alkyne to close the heterocyclic ring.
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro- 1-hydroxy-2,1-benzoxaborole (AN2690), for the potential treatment of onychomycosis
Baker, Stephen J.,Zhang, Yong-Kang,Akama, Tsutomu,Lau, Agnes,Zhou, Huchen,Hernandez, Vincent,Mao, Weimin,Alley,Sanders, Virginia,Plattner, Jacob J.
, p. 4447 - 4450 (2007/10/03)
A structure-activity relationship investigation for a more efficacious therapy to treat onychomycosis, a fungal infection of the toe and fingernails, led to the discovery of a boron-containing small molecule, 5-fluoro-1,3-dihydro- 1-hydroxy-2,1-benzoxaborole (AN2690), which is currently in clinical trials for onychomycosis topical treatment.