- A New Convenient Synthesis of Dialkyl(methylene)ammonium Chloride
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A new, convenient synthesis of dialkyl(methylene)ammonium chloride is proposed from gem-aminoethers and methyltrichlorosilane, a by-product of the industrial methylchlorosilane synthesis.
- Rochin, C.,Babot, O.,Dunogues, J.,Duboudin, F.
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- Synthesis of: N -[(dialkylamino)methyl]acrylamides and N -[(dialkylamino)methyl]methacrylamides from Schiff base salts: Useful building blocks for smart polymers
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The traditional thermal Mannich reaction is unsuitable for preparing polymerizable N-methylene amino substituted acrylamides and methacrylamides. Herein we provide a facile multi-gram high yield synthesis of these monomeric precursors to stimuli-responsive polymers by the addition of acrylamides and methacrylamides onto in situ generated or freshly isolated methylene Schiff base (iminium) salts. The X-ray crystal structure of the hydrated iminium salt, 1-(hydroxymethyl)azocan-1-ium chloride and monomer·HCl salt (N-[(azocan-1-yl)methyl]prop-2-enamide hydrochloride) is described.
- Alzahrani, Abdullah,Mirallai, Styliana I.,Chalmers, Benjamin A.,McArdle, Patrick,Aldabbagh, Fawaz
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p. 4108 - 4116
(2018/06/12)
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- Substituted Sulfonamide Compounds
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Substituted sulfonamide compounds corresponding to the formula I wherein m, n, p, Q, R1, R2, R3, R4, X, Y and Z have the respective meanings defined herein, pharmaceutical compositions containing such compounds, a process for their preparation, and the use of such compounds for the treatment and/or inhibition of pain and other conditions mediated by bradykinin receptor 1 (B1R) and/or bradykinin receptor 2 (B2R).
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Page/Page column 36-37
(2009/07/25)
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- SUBSTITUTED SULFONAMIDE DERIVATIVES
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The invention relates to substituted sulfonamide derivatives of the general formula (I'); processes for their preparation, medicaments containing these compounds, and the use of substituted sulfonamide derivatives for the preparation of medicaments
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Page/Page column 110
(2009/08/16)
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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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- MANNICH REACTIONS OF ARYLTRIALKYLSTANNANES IN APROTIC SOLVENTS
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Aryltributyl- and aryltrimethyl-stannanes react with a range of N,N-dialkylmethylene-imonium salts to afford N,N-dialkylaminomethyl derivatives in good yields.The method can be used to obtain regioisomers that are not available using classical procedures. "In situ" reactions can also be carried out using alkoxydialkylaminomethanes (aminol ethers) and bis(dialkylamino)methanes (aminals) together with chlorotrimethyl- and trichloromethyl-silanes as the source of the electrophile.However, the "in situ" reactions do not afford good yields in the majority of cases, as a result of the inhibition of imonium salt formation by trialkylchlorostannane.
- Cooper, Mark S.,Fairhurst, Robin A.,Heaney, Harry,Papageorgiou, George,Wilkins, Robert F.
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p. 1155 - 1166
(2007/10/02)
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- MANNICH REACTIONS OF FURAN AND 2-METHYLFURAN USING PRE-FORMED IMONIUM SALTS
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Good yields of 2-dialkylaminomethylfurans are obtained when N,N-dialkylmethylene-imonium chlorides are allowed to interact with furan in acetonitrile at room temperature; similar results are obtained using 2-methylfuran.
- Heaney, Harry,Papageorgiou, George,Wilkins, Robert F.
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p. 2377 - 2380
(2007/10/02)
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- 3-(Substituted aminomethyl)-7-substituted-3,5-dihydro-as-triazino[4,3-a][1,5]benzodiazepines
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A compound of the formula: SPC1 Wherein R, R0, and R3 are hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; wherein R1 and R2 are alkyl of 1 to 3 carbon atoms, or the group EQU1 together is pyrrolidino, piper
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