- Metal-free synthesis of β-aminoketones by the reductive hydroamination of ynones
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This study describes a cascade method for the synthesis of β-aminoketones through the reductive hydroamination of alkynes under very mild metal-free conditions. It allows for the rapid conversion of ynones and amines into corresponding β-aminoketones with a broad substrate scope and diverse functionalities. This straightforward and easy-to-handle reaction process can be successfully applied for the synthesis of Proroxan and Propipocaine, offering a potential option for the synthesis of drug molecules with the β-aminoketone skeleton.
- Fu, Rui,Liu, Yu,Wu, Tao,Zhang, Xinyu,Zhu, Yang,Luo, Jiangbin,Zhang, Zhengyu,Jiang, Yaojia
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p. 3525 - 3528
(2022/03/31)
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- Evaluation of Cytotoxic Properties of N,N'-bis[(1-aryl-3-heteroaryl)propylidene]-hydrazine dihydrochlorides
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N,N'-bis[(1-aryl-3-heteroaryl)propylidene]hydrazine dihydrochlorides, P1, P4 – P8, and R1 – R7, were assayed against human oral squamous cell carcinoma (HSC-2, HSC-3, HSC-4), human promyelocytic leukemia cell line (HL-60), and human normal oral cells (HGF
- Kucukoglu,Gul,Sakagami
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p. 784 - 787
(2020/11/23)
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- Electrooxidative cyclization of hydroxyamino compounds possessing a benzyl group
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Several novel 2-aryl-1,3-oxazinane and 2-aryl-1,3-oxazolidine derivatives were synthesized from N-benzyl-2-piperidineethanols and N-benzyl-2- piperidinemethanols, respectively, by using electrooxidative methods in methanol. For these reactions, the yields of the corresponding cyclized compounds were significantly increased by using catalytic amounts of iodide ions. In contrast, 3-dialkylamino-1-phenylpropanols afforded the expected cyclic 6-phenyl-1,3-oxazinane derivatives using only a small excess of base. Georg Thieme Verlag Stuttgart · New York.
- Okimoto, Mitsuhiro,Ohashi, Kousuke,Yamamori, Haruki,Nishikawa, Shinnosuke,Hoshi, Masayuki,Yoshida, Takashi
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experimental part
p. 1315 - 1322
(2012/06/30)
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- Hypolipidemic effects of α, β, and γ-alkylaminophenone analogs in rodents
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A number of N-substituted β-alkylaminophenone derivatives including two (α- and two γ-alkylaminophenone analogs were synthesized and investigated for hypolipidemic activity in mice at 8 mg/kg/day ip. Most of these analogs were found to be significantly more active than lovastatin and clofibrate. N-Phenylpiperazinopropiophenone 16 was one of the best derivatives, lowering serum cholesterol levels 41% and serum triglyceride levels 48% after 16 days of drug administration in CF1 mice. In Sprague-Dawley rats, N-phenylpiperazinopropiophenone at 8 mg/kg/day orally also demonstrated more potent hypolipidemic activity than clofibrate, gemfibrozil, and lovastatin at their therapeutic dosage. It significantly reduced tissue cholesterol and triglyceride levels in the aorta wall tissue and lowered the cholesterol and triglyceride levels in chylomicron, very low density lipid (VLDL) and low density lipid (LDL) fractions, while it significantly elevated the cholesterol levels in high density lipid (HDL) fraction. This compound also proved to be active in lowering both cholesterol and triglyceride levels in hyperlipidemic mice and rats induced with atherogenic diet. In vitro liver acetyl coenzyme A (CoA) synthetase, 3-hydroxy-3-methyl glutaryl (HMG) CoA reductase, acyl CoA cholesterol acyl transferase (ACAT), sn-glycerol-3-phosphate acyltransferase, phosphatidylate phosphohydrolase, and hepatic lipoprotein lipase activities were significantly inhibited by N-phenylpiperazinopropiophenone from 25 to 100 μM.
- Huang,Hall
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p. 281 - 290
(2007/10/03)
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- Synthesis of 3-aryloxy-3-phenylpropanamines as possible antidepressants
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Thirteen new 3-aryloxy-3-phenylpropanamines (11-23) have been prepared and their structures elucidated by mass, IR and 1H-NMR spectra and by elemental analysis.Being structurally similar to fluoxetine these compounds have been tested for their effect on g
- Sharma. V. L.,Bhandari, Kalpana,Chatterjee, S. K.,Satyanarayana, K. V.,Dua, P. R.
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p. 393 - 396
(2007/10/02)
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- Carbon-Carbon Bond Formation by the Use of Chloroiodomethane as a C1 Unit. IV. The Mannich Reaction of Ketones by Means of Dihalomethane and Secondary Amine
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Treatment of ketones with dihalomethane (CH2Br2, CH2ClI, and CH2I2) in the presence of secondary amine, preferably pyrrolidine, gave the corresponding Mannich base in varing yields depending on the substrate and/or combination of the reagents.
- Miyano, Sotaro,Mori, Akira,Hokari, Hiroshi,Ohta, Katsuaki,Hashimoto, Harukichi
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p. 1331 - 1332
(2007/10/02)
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