59500-67-3Relevant academic research and scientific papers
Metal- and radical-free aerobic oxidation of heteroaromatic methanes: An efficient synthesis of heteroaromatic aldehydes
Ye, Rongzi,Cao, Yuanjie,Xi, Xiaoxiang,Liu, Long,Chen, Tieqiao
supporting information, p. 4220 - 4224 (2019/05/10)
A metal-free and radical-free synthesis of heteroaromatic aldehydes was developed through aerobic oxidation of methyl groups in an I2/DMSO/O2 catalytic system. Under the reaction conditions, various functional groups such as methoxy, aldehyde, ester, nitro, amide, and halo (F, Cl, Br) groups were well tolerated. The bioactive compounds like chlorchinaldin derivative and papaverine were also oxidized to the corresponding aldehydes and ketones. This reaction provided an efficient method for preparing the valuable heteroaromatic aldehydes.
Chemical synthesis method of quinoline (oxaline)-2-carboxaldehyde compounds
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Paragraph 0056-0058, (2017/04/14)
The invention relates to a preparation method of quinoline (oxaline)-2-carboxaldehyde compounds. The preparation method comprises the following steps of dissolving 2-methylquinoline(oxaline) shown in a formula (II) into an organic solvent, adding iron salts, and completely reacting under the condition of 100 to 180DEG C with the assistance of microwave; performing after treatment on a reaction solution to obtain the quinoline (oxaline)-2-carboxaldehyde compounds shown in a formula (I), wherein the feed molar ratio of the iron salts to the quinoline (oxaline)-2-carboxaldehyde compounds is (0.5 to 3.5):1. R in the formula (I) and the formula (II) is hydrogen at the same time; or the hydrogen is monosubstituted or polysubstituted by alkyls of C1 to C8, alkoxys of C1 to C8, nitryl or halogen; the number of substituent groups is n; X in the formula (I) and the formula (II) is carbon or nitrogen at the same time. The preparation method disclosed by the invention has the advantages of short reaction time, low reaction temperature, wide application range of reaction, good reaction selectivity, low price and no toxicity of a used catalyst, and simplicity and convenience in operation; the preparation method meets the requirement of green chemistry. (The formulas are shown in the description).
Metal-free C(sp3)–H oxidation of 2-methylquinolines with PIDA under microwave irradiation
Jiang, Long,Huang, Yingyi,Yan, Yiyan,Xie, Yuanyuan
supporting information, p. 4149 - 4151 (2016/08/24)
An efficient metal-free protocol has been developed for the sp3C–H bond oxidation of 2-methylquinolines in the presence of PIDA under microwave irradiation, providing 2-quinolinecarboxaldehydes with moderate to high yields and excellent selectivities. A wide range of 2-quinolinecarboxaldehydes with different functional groups have been synthesized. A tentative mechanism has been presented to explain this highly selective oxidation process.
Phenanthro[9,10-d ]imidazole-quinoline boron difluoride dyes with solid-state red fluorescence
Li, Weiling,Lin, Weiying,Wang, Jiaoliang,Guan, Xiaoyu
supporting information, p. 1768 - 1771 (2013/07/05)
A new family of boron difluoride-rigidified dyes, phenanthro[9,10-d] imidazole-quinoline boron difluoride (PQBD), with solid-state fluorescence has been designed and synthesized. The novel series of PQBD are advantageous over the typical boron difluoride-rigidified dyes such as BODIPYs in terms of large Stokes shift and red fluorescence in the solid state.
Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1
Tavares, Francis X.,Al-Barazanji, Kamal A.,Bigham, Eric C.,Bishop, Michael J.,Britt, Christy S.,Carlton, David L.,Feldman, Paul L.,Goetz, Aaron S.,Grizzle, Mary K.,Guo, Yu C.,Handlon, Anthony L.,Hertzog, Donald L.,Ignar, Diane M.,Lang, Daniel G.,Ott, Ronda J.,Peat, Andrew J.,Zhou, Hui-Qiang
, p. 7095 - 7107 (2008/04/18)
The high expression of MCH in the hypothalamus with the lean hypophagic phenotype coupled with increased resting metabolic rate and resistance to high fat diet-induced obesity of MCH KO mice has spurred considerable efforts to develop small molecule MCHR1 antagonists. Starting from a lead thienopyrimidinone series, structure-activity studies at the 3- and 6-positions of the thienopyrimidinone core afforded potent and selective MCHR1 antagonists with representative examples having suitable pharmacokinetic properties. Based on structure-activity relationships, a structural model for MCHR1 was constructed to explain the binding mode of these antagonists. In general, a good correlation was observed between pKas and activity in the right-hand side of the template, with Asp123 playing an important role in the enhancement of binding affinity. A representative example when evaluated chronically in diet-induced obese mice resulted in good weight loss effects. These antagonists provide a viable lead series in the discovery of new therapies for the treatment of obesity.
Heterocyclic mchr1 antagoists
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Page/Page column 31, (2010/11/24)
This invention relates to novel heterocycles which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), also referred to as 11 CBy, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in
Novel lipopeptides as antibacterial agents
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, (2008/06/13)
The present invention relates to novel lipopeptide compounds. The invention also relates to pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The invention also relates to methods of producing
