59171-72-1Relevant academic research and scientific papers
Substituted N - ((1 °, 3° - [...] - 4° - yl) - methyl) - 4 - benzoyl piperidine compound and use thereof
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Paragraph 0088; 0089; 0090; 0104; 0105; 0106, (2017/04/29)
The invention discloses a substituted N-((1', 3'-azole-4'-yl)-methyl)-4-benzoyl-hexahydropyridine compound represented by formula I, a preparation method thereof, and applications of the substituted N-((1', 3'-oxazole-4'-yl)-methyl)-4-benzoyl-hexahydropyridine compound in preparation of antituberculous drugs. The substituted N-((1', 3'-azole-4'-yl)-methyl)-4-benzoyl-hexahydropyridine compound possesses activity on mycobacterium tuberculosis-susceptible strains, and also possesses activity on strains with tolerance on traditional first-line antituberculous drugs such as isoniazide and rifampicin, and is a novel mycobacterium tuberculosis resistant compound with a promising application prospect.
Towards New Tricyclic Motifs: Intramolecular C–H Arylation as the Key Step in a Formal [3+3] Cyclocondensation Strategy
Vrijdag, Johannes L.,De Ruysscher, Dries,De Borggraeve, Wim M.
, p. 1465 - 1474 (2017/04/01)
Tricyclic scaffolds structurally related to the well-known benzodiazepine class of drugs show diverse biological activities strikingly different from those of their benzodiazepine counterparts. Interested by this scaffold-hopping perspective, we previousl
The rapid synthesis of oxazolines and their heterogeneous oxidation to oxazoles under flow conditions
Gl?ckner, Steffen,Tran, Duc N.,Ingham, Richard J.,Fenner, Sabine,Wilson, Zoe E.,Battilocchio, Claudio,Ley, Steven V.
, p. 207 - 214 (2015/02/02)
A rapid flow synthesis of oxazolines and their oxidation to the corresponding oxazoles is reported. The oxazolines are prepared at room temperature in a stereospecific manner, with inversion of stereochemistry, from β-hydroxy amides using Deoxo-Fluor. The
I2-Catalyzed C-O Bond Formation and Dehydrogenation: Facile Synthesis of Oxazolines and Oxazoles Controlled by Bases
Gao, Wen-Chao,Hu, Fei,Huo, Yu-Ming,Chang, Hong-Hong,Li, Xing,Wei, Wen-Long
supporting information, p. 3914 - 3917 (2015/08/18)
A general method for the synthesis of oxazolines and oxazoles was developed through I2-catalyzed C-O bond formation and dehydrogenation with the same oxidant, TBHP. By simply tuning reaction bases, either oxazolines or oxazoles were selectively
Discovery of the disubstituted oxazole analogues as a novel class anti-tuberculotic agents against MDR- and XDR-MTB
Li, Dongsheng,Gao, Nana,Zhu, Ningyu,Lin, Yuan,Li, Yan,Chen, Minghua,You, Xuefu,Lu, Yu,Wan, Kanglin,Jiang, Jian-Dong,Jiang, Wei,Si, Shuyi
supporting information, p. 5178 - 5181 (2015/11/09)
A high-throughput screening effort on 45,000 compounds resulted in the discovery of a disubstituted oxazole as a new structural class inhibitor of Mycobacterium tuberculosis (Mtb). In order to improve the activity and investigate the SAR of this scaffold, a series of disubstituted azole analogues have been designed and synthesized. The newly synthesized compounds 1a-y were evaluated for their in vitro anti-TB activity versus replicating, multi- and extensive drug resistant Mtb strains. All the compounds, except 1o, 1p and 1q, showed potent anti-TB activity with MIC of 1-64 mg/L. The test of broad spectrum panel revealed that this series are specific to Mtb. The cytotoxicity assessment indicated that the compounds were not cytotoxic against HEK 293 cells. The compounds could have a novel mechanism to anti-Mtb as they can inhibit drug sensitive and drug resistant Mtb.
Convenient Synthesis of Azolines to Azoles
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Paragraph 0102; 0110, (2013/03/26)
Azolines are oxidized in the presence of a copper-containing catalyst to azoles in the presence of molecular oxygen. A synthetic scheme converting azolines azoles is also provided.
Copper-catalyzed oxidation of azolines to azoles
Dawsey, Anna C.,Li, Vincent,Hamilton, Kimberly C.,Wang, Jianmei,Williams, Travis J.
experimental part, p. 7994 - 8002 (2012/08/08)
We report herein convenient, aerobic conditions for the oxidation of thiazolines to thiazoles and data regarding the oxidation mechanism. These reactions feature operationally simple and environmentally benign conditions and proceed in good yield to afford the corresponding azoles, thus enabling the inexpensive preparation of valuable molecular building blocks. Incorporation of a novel diimine-ligated copper catalyst, [(MesDABMe) CuII(OH2)3]2+ [-OTf] 2, provides increased reaction efficiency in many cases. In other cases copper-free conditions involving a stoichiometric quantity of base affords superior results.
Pd(ii)-catalyzed direct C5-arylation of azole-4-carboxylates through double C-H bond cleavage
Li, Ziyuan,Ma, Ling,Xu, Jinyi,Kong, Lingyi,Wu, Xiaoming,Yao, Hequan
supporting information; scheme or table, p. 3763 - 3765 (2012/06/15)
The first palladium-catalyzed direct C5-arylation of azole-4-carboxylates with simple unactivated arenes through double C-H bond cleavage is realized. This protocol provided a straightforward access to diverse 5-arylsubstituted azole-4-carboxylic derivatives with good functional group tolerance. The Royal Society of Chemistry 2012.
Hydroxamic Acids as Potent Inhibitors of FeII and MnII E. coli Methionine Aminopeptidase: Biological Activities and X-ray Structures of Oxazole Hydroxamate-EcMetAP-Mn Complexes
Huguet, Florian,Melet, Armelle,Alves de Sousa, Rodolphe,Lieutaud, Aurelie,Chevalier, Jacqueline,Maigre, Laure,Deschamps, Patrick,Tomas, Alain,Leulliot, Nicolas,Pages, Jean-Marie,Artaud, Isabelle
, p. 1020 - 1030 (2012/07/31)
New series of acids and hydroxamic acids linked to five-membered heterocycles including furan, oxazole, 1,2,4- or 1,3,4-oxadiazole, and imidazole were synthesized and tested as inhibitors against the FeII, CoII, and MnII f
Copper(II)-catalyzed oxidation of 4-carboxythiazolines and 4-carboxyoxazolines to 4-carboxythiazoles and 4-carboxyoxazoles
Wang, Yiyun,Li, Ziyuan,Huang, Yue,Tang, Changhua,Wu, Xiaoming,Xu, Jinyi,Yao, Hequan
supporting information; experimental part, p. 7406 - 7411 (2011/10/09)
A mild copper(II)-catalyzed oxidation of 4-carboxythiazolines and 4-carboxyoxazolines to 4-carboxythiazoles and 4-carboxyoxazoles has been developed. Various substrates with alkyl or aryl substitutions at 2-position on azoline ring could be smoothly oxidi
