142978-20-9Relevant articles and documents
Silyl modification of biologically active compounds. 4. Derivatives of amino acids in the tetrahydroquinoline, tetrahydroisoquinoline, and tetrahydrosilaisoquinoline series
Lukevics,Germane,Segal,Zablotskaya
, p. 234 - 238 (1997)
A series of derivatives of (1,2,3,4-tetrahydro-1-quinolyl)-, (1,2,3,4-tetrahydro-2-isoquinolyl)-, and (1,2,3,4-tetrahydrosila-2-isoquinolyl)acetic acid, which are structural analogs of glycine, were synthesized. The psychotropic activity and the acute toxicity of the compounds were studied. 1997 Plenum Publishing Corporation.
A facile one-pot synthesis of N-substituted tetrahydroquinolines
Babu, Thelagathoti Hari,Shanthi, Gnanamani,Perumal, Paramasivan T.
, p. 2881 - 2884 (2009)
An uncatalyzed one-pot synthesis of N-substituted tetrahydroquinolines was achieved in good yields by the reaction of quinoline and alkyl/acyl halides with Hantzsch dihydropyridine ester under mild reaction conditions.
Photoredox-Catalyzed α-Aminomethyl Carboxylation of Styrenes with Sodium Glycinates: Synthesis of γ-Amino Acids and γ-Lactams
Zhou, Cong,Li, Miao,Sun, Jianwei,Cheng, Jiang,Sun, Song
supporting information, p. 2895 - 2899 (2021/05/05)
A visible-light photoredox-catalyzed reductive α-aminomethyl carboxylation of styrenes with sodium glycinates and CO2 has been developed to synthesize a series of α,α-disubstituted γ-amino acids and γ-lactams with high efficiency and regioselectivity. Notably, CO2 released from the decarboxylation step can be reused for the subsequent carboxylation. Distinct from the previous reactions with the same type of substrates leading to simple decarboxylation and olefin hydroalkylation, this process involves additional CO2 sequestration, thus leading to olefin α-aminomethyl carboxylation. These findings not only provide new access to α,α-disubstituted γ-amino acids and γ-lactams but also serve as a proof of concept for CO2 reutilization in decarboxylation reactions.
Arylamino containing hydroxamic acids as potent urease inhibitors for the treatment of Helicobacter pylori infection
Liu, Qi,Shi, Wei-Kang,Ren, Shen-Zhen,Ni, Wei-Wei,Li, Wei-Yi,Chen, Hui-Min,Liu, Pei,Yuan, Jing,He, Xiao-Su,Liu, Jia-Jia,Cao, Peng,Yang, Pu-Zhen,Xiao, Zhu-Ping,Zhu, Hai-Liang
, p. 126 - 136 (2018/07/13)
A novel series of aniline-containing hydroxamic acids were designed, synthesized and evaluated as anti-virulence agents for the treatment of gastritis and gastric ulcer caused by Helicobacter pylori. In vitro enzyme-based screen together with in vivo assays and structure?activity relationship (SAR) studies led to the discovery of three potent urease inhibitors 3-(3,5-dichlorophenylamino)–N-hydroxypropanamide (3a), 3-(2-chlorophenylamino)–N-hydroxypropanamide (3d) and 3-(2,4-dichlorophenylamino)–N-hydroxypropanamide (3n). Compounds 3a, 3d and 3n showed excellent urease inhibition with IC50 values 0.043 ± 0.005, 0.055 ± 0.008 and 0.018 ± 0.002 μM, and significantly depressed gastritis developing at the dose of 32 mg/kg b. i.d with eradication rates of H. pylori reaching 92.3, 84.6 and 100%, respectively. Preliminary safety studies (acute toxicity in mice) disclosed that 3a, 3d and 3n was well-tolerated in KM mice with LD50s of 2982.8, 3349.4 and 3126.9 mg/kg, respectively. Collectively, the data obtained in this study indicate that 3a, 3d and 3n, in particular 3n, could considered as promising candidates for the potential treatment of H. pylori caused gastritis and gastric ulcer, and hence merit further studies.
Method for synthesizing alpha-amino-acid ester compound through catalytic oxidation one-step process
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Paragraph 0090; 0091; 0097, (2017/09/01)
The invention belongs to the technical field of organic chemical industry and discloses a method for synthesizing an alpha-amino-acid ester compound through a catalytic oxidation one-step process. The method comprises the following steps: (1) reacting a vinyl ether/amine compound or alkene amide compound with an amine compound in an organic solvent under a synergic effect of a catalyst and an oxidizing agent; and (2) separating and purifying a product after the ending of the reaction, thereby acquiring the alpha-amino-acid ester compound. The method is simple and safe in operation, the compound is synthesized within one step, an ester bond is acquired in a reaction process, a nontoxic pollution-free peroxide is used as an oxidizing agent, the raw materials are low in cost and are easily acquired and the alpha-amino-acid ester compound has wide adaptability to functional groups, wide adaptability to substrates, environmental protection and an excellent industrial application prospect.
Access to α-Amino Acid Esters through Palladium-Catalyzed Oxidative Amination of Vinyl Ethers with Hydrogen Peroxide as the Oxidant and Oxygen Source
Ouyang, Lu,Li, Jianxiao,Zheng, Jia,Huang, Jiuzhong,Qi, Chaorong,Wu, Wanqing,Jiang, Huanfeng
supporting information, p. 15926 - 15930 (2017/11/23)
A novel and convenient palladium catalytic system for the synthesis of α-amino acid esters from simple starting materials is reported. Hydrogen peroxide not only acts as the green oxidant, but also as the oxygen source. This strategy for the conversion of amines and vinyl ethers into highly functionalized and structurally diverse α-amino acid esters is characterized by the simplicity of the experimental procedure, mild reaction conditions, high atom economy, scalability, and practicability.
CURE ACCELERATORS FOR ANAEROBIC CURABLE COMPOSITIONS
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Paragraph 0086, (2017/07/14)
Cure accelerators for anaerobic curable compositions, such as adhesives and sealants, are provided, and which are defined with reference to the compounds shown in structure I where A is CH2 or benzyl, R is C1-10 alkyl, R′ is H or Cs
4-(Benzoimidazol-2-yl)-thiazole Compounds and Related Aza Derivatives
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Paragraph 0773, (2015/01/06)
The invention relates to compounds of Formula (I) wherein ring A, X, (R1)n, R2, R3, R4, R4′, R5, n, and p are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.
4-(BENZOIMIDAZOL-2-YL)-THIAZOLE COMPOUNDS AND RELATED AZA DERIVATIVES
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Page/Page column 104, (2013/08/15)
The invention relates to compounds of Formula (I) wherein ring A, X, (R1)n, R2, R3, R4, R4', R5, n, and p are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4- dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors
Zhang, Jing,Zhan, Peng,Wu, Jingde,Li, Zhenyu,Jiang, Yan,Ge, Weiying,Pannecouque, Christophe,De Clercq, Erik,Liu, Xinyong
experimental part, p. 4366 - 4376 (2011/08/09)
A series of novel S-DABO analogues of 5-alkyl-2-arylthio-6-((3,4- dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Among them, the most potent HIV-1 inhibitor
