532-24-1Relevant articles and documents
Bioactivity-guided synthesis of tropine derivatives as new agonists for melatonin receptors
Yin, Xiu-Juan,Geng, Chang-An,Huang, Xiao-Yan,Chen, Hao,Ma, Yun-Bao,Chen, Xing-Long,Sun, Chang-Li,Yang, Tong-Hua,Zhou, Jun,Zhang, Xue-Mei,Chen, Ji-Jun
, p. 45059 - 45063 (2016)
Twenty-three tropine derivatives as new melatonin receptor (MT1 and MT2) agonists were synthesized and evaluated on HEK293 cells in vitro. Derivatives 1f, 1i, 1j, 1m-1s and 1t exhibited increased agonisting activities on MT1 and MT2 receptors compared to the substrate tropine. Particularly, compound 1r showed significant agonistic activities on MT1 and MT2 receptors with EC50 values of 0.20 and 0.24 mM, respectively. The preliminary structure-activity relationships (SARs) of tropine derivatives were summarized for further investigation on melatonin receptor agonists.
N-Methylation of Amines with Methanol at Room Temperature
Tsarev, Vasily N.,Morioka, Yuna,Caner, Joaquim,Wang, Qing,Ushimaru, Richiro,Kudo, Akihiko,Naka, Hiroshi,Saito, Susumu
supporting information, p. 2530 - 2533 (2015/05/27)
N-Methylation of amines with methanol proceeds at room temperature in the presence of a silver-loaded titanium dioxide (Ag/TiO2) photocatalyst under UV-vis light irradiation. This method allows facile synthesis/isolation of N-methylamines bearing various functional groups including N-benzyl, N-allyl, N-Boc, hydroxyl, ether, acetal, carboxamide, formamide, and olefin groups. (Chemical Presented)
METHOD OF PRODUCING TERTIARY AMINE OR TERTIARY AMINE DERIVATIVE
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Paragraph 0066; 0073; 0079, (2018/10/31)
PROBLEM TO BE SOLVED: To provide a method of producing tertiary amine or tertiary amine derivative with high selectivity. SOLUTION: In the method of producing tertiary amine or tertiary amine derivative, a reaction system including: an organic chemical raw material containing at least one kind of group selected from -NH2, -NH2 HCl, >NH and >NH HCl, a nitrogen atom contained in the group bounding to a carbon atom; aliphatic alcohol having 1 to 20 carbon atoms; and a catalyst where a carrier containing titanium oxide carries a silver component (metal silver or silver compound), is irradiated with light, and the group in the organic compound raw material is converted to -NR02 or >NR0, ( R0 is an aliphatic hydrocarbon group having 1 to 20 carbon atoms derived from the aliphatic alcohol). The percentage content of the silver in the catalyst is 0.5 to 10 mass% with respect to the titanium oxide. COPYRIGHT: (C)2015,JPOandINPIT
CRYSTALLINE ATROPINE SULFATE
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Page/Page column 4, (2014/07/21)
The present invention relates to crystalline polymorph form of Atropine sulfate and process for the preparation thereof.
A facile synthesis of enantiopure 7-benzyloxycarbonyl-7-azabicyclo [2.2.1]heptane-2-carboxylic acid
Chiou, Wen-Hua,Chiang, Yu-Min,Chen, Guei-Tang
, p. 92 - 97 (2014/02/14)
An efficient procedure for the preparation of enantiopure 7-benzyloxycarbonyl-7-azabicyclo[2.2.1]heptane-2-carboxylic acids is described.
Total synthesis of tropinone using 1,3-dipolar cycloaddition of cyclic azomethine ylide and phenyl vinyl sulfone as the key step
Laha, Joydev K.
experimental part, p. 254 - 256 (2010/09/18)
Total synthesis of tropinone from the readily available piperidone 2 is described. The rapid assembly of the tropane skeleton was achieved by 1,3-dipolar cycloaddition of cyclic azomethine ylide 3 to phenyl vinyl sulfone.
Productive chloroarene C-Cl bond activation: Palladium/phosphine-catalyzed methods for oxidation of alcohols and hydrodechlorination of chloroarenes
Bei, Xiaohong,Hagemeyer, Alfred,Volpe, Anthony,Saxton, Robert,Turner, Howard,Guram, Anil S.
, p. 8626 - 8633 (2007/10/03)
The palladium/phosphine-catalyzed productive chloroarene C-Cl bond activation provides general, efficient, and functional group friendly methods for the selective oxidation of alcohols and the hydrodechlorination of chloroarenes.
Iodine(V) reagents in organic synthesis. Part 4. o-Iodoxybenzoic acid as a chemospecific tool for single electron transfer-based oxidation processes
Nicolaou,Montagnon,Baran,Zhong
, p. 2245 - 2258 (2007/10/03)
o-Iodoxybenzoic acid (IBX), a readily available hypervalent iodine(V) reagent, was found to be highly effective in carrying out oxidations adjacent to carbonyl functionalities (to form α, β-unsaturated carbonyl compounds) and at benzylic and related carbon centers (to form conjugated aromatic carbonyl systems). Mechanistic investigations led to the conclusion that these new reactions are initiated by single electron transfer (SET) from the substrate to IBX to form a radical cation which reacts further to give the final products. Fine-tuning of the reaction conditions allowed remarkably selective transformations within multifunctional substrates, elevating the status of this reagent to that of a highly useful and chemoselective oxidant.
Novel asymmetric dealkoxycarbonylation of 3-oxo-8-azabicyclo[3.2.1]- octane-2,4-dicarboxylates using porcine liver esterase: A new route to (-)- anhydroecgonine methyl ester
Node, Manabu,Nakamura, Soichi,Nakamura, Daisaku,Katoh, Takahiro,Nishide, Kiyoharu
, p. 5357 - 5360 (2007/10/03)
The porcine liver esterase-catalyzed dealkoxycarbonylation of 8-benzyl- 3-oxo-8-azabicyclo[3.2.1]octane-2,4-dicarboxylates (4) was found to give high enantiomeric excess of the desymmetrized keto ester (5). This novel dealkoxylcarbonylation opened a new route to the asymmetric synthesis of (1R)-cocaine related radiopharmaceuticals such as (1R)-β-CIT, for diagnosis of Parkinson's disease.
