- Thymol, and preparation method and pharmaceutical composition thereof
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The invention discloses thymol, and a preparation method and pharmaceutical composition thereof. The preparation method comprises the steps of: conducting a condensation reaction on m-cresol and ethylacetoacetate to obtain 4,7-dimethylcoumarin, performing hydrolysis decarboxylation on the 4,7-dimethylcoumarin under conditions of a strong alkali and high temperature to obtain an organic phase C containing 5-methyl-2-(prop-1-en-2-yl)phenol, and reducing the organic phase C to obtain thymol. The preparation method of thymol disclosed by the invention is mild in conditions, does not need specialreaction equipment, and facilitates industrial production. With the preparation method, position selectivity is high, almost no position isomer is generated, the separated product is high in purity, the total yield is high and the product quality accords with current drug declaration requirements.
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- Total Synthesis of a Dimeric Thymol Derivative Isolated from Arnica sachalinensis
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The total synthesis of a dimeric thymol derivative (thymarnicol) isolated from Arnica sachalinensis was accomplished in 6 steps. A key biomimetic Diels–Alder dimerization was found to occur at ambient temperature and the final oxidative cyclization occurs
- De Silvestro, Irene,Drew, Samuel L.,Nichol, Gary S.,Duarte, Fernanda,Lawrence, Andrew L.
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supporting information
p. 6813 - 6817
(2017/06/06)
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- Synthesis of coumarins via Pd-catalyzed oxidative cyclocarbonylation of 2-vinylphenols
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Palladium-catalyzed oxidative cyclocarbonylation of 2-vinylphenols constitutes a simple, direct method for the synthesis of coumarins. The reaction conditions, employing low pressures of CO, and air or 1,4- benzoquinone as the oxidant, are attractive in terms of environmental considerations and operational simplicity. Coumarins with a variety of functional groups were prepared in yields up to 85%.
- Ferguson, Jamie,Zeng, Fanlong,Alper, Howard
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supporting information
p. 5602 - 5605,4
(2012/12/12)
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- Ethylene glycol as hydrogen donor for the syntheses of thymol analogues via hydrolysis of 4-methylcoumarins
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Treatment of 4-methylcoumarins with potassium hydroxide in ethylene glycol resulted in the formation of the 'normal' 2-isopropenylphenols and/or the 'abnormal' 2-isopropylphenols depending on the nature of the substrates. The solvent ethylene glycol was b
- Chang, Junbiao,Wang, Shuyang,Shen, Zhenhua,Huang, Gang,Zhang, Yueteng,Zhao, Jing,Li, Changwei,Fan, Fangfang,Song, Chuanjun
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supporting information
p. 6755 - 6757,3
(2012/12/12)
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- A simple synthesis of 4H-1,3-benzodioxin-2-one derivatives by iodocyclization of t-butyl o-vinylphenyl carbonate derivatives
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The first general method for the synthesis of 4H-1,3-benzodioxin-2-one derivatives has been developed. Treatment of t-butyl 2-vinylphenyl carbonates with iodine in the presence of sodium hydrogencarbonate gave 4-iodomethyl-4H-1,3-benzodioxin-2-one derivat
- Kobayashi, Kazuhiro,Nakamura, Daizo,Miyamoto, Kazuna,Morikawa, Osamu,Konishi, Hisatoshi
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p. 489 - 491
(2007/10/03)
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- Characterization of a series of 3-amino-2-phenylpropene derivatives as novel bovine chromaffin vesicular monoamine transporter inhibitors
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A series of 3-amino-2-phenylpropene (APP) derivatives have been synthesized and characterized as novel competitive inhibitors, with Ki values in the μM range, for the bovine chromaffin granule membrane monoamine transporter(s) (bVMAT). Although, these inhibitors are structurally similar to the bVMAT substrate tyramine, none of them were measurably transported into the granule. Structure - activity studies have revealed that, while the 3′- or 4′-OH groups on the aromatic ring enhance the inhibition potency, Me or OMe groups in these positions reduce the inhibition potency. Halogen substitution on the 4′-position of the aromatic ring causes gradual increase of the inhibition potency parallel to the electron donor ability of the halogen. Substituents on the NH2 as well as on the 3-position of the alkyl chain reduce the inhibition potency. Comparative structure - activity analyses of APP derivatives with tyramine and the neurotoxin 1-methyl-4-phenylpyridinium suggest that the flexibility of the side chain and the relative orientation of the NH2 group may be critical for the efficient transport of the substrate through the bVMAT. Comparable bVMAT affinities of these inhibitors to that of DA and other pharmacologically active amines suggest that they are suitable for the structure activity and mechanistic studies of monoamine transporters and may also be useful in modeling the mechanism of action of amphetamine-related derivatives.
- Perera, Rohan P.,Wimalasena, D. Shyamali,Wimalasena, Kandatege
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p. 2599 - 2605
(2007/10/03)
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- Formal syntheses of heliannuols A and D, allelochemicals from Helianthus annus
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A synthesis of heliannuol A 1 is described involving hydrogenolysis of the cyclopropane fused benzoxepane compound 23 to generate the benzoxocane ring system of 1 and a fragmentation of methyl ether 25 furnished 4-methoxycurcuphenol 29, an advanced interm
- Tuhina, Kazi,Bhowmik, Dipal R.,Venkateswaran, Ramanathapuram V.
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p. 634 - 635
(2007/10/03)
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- A SHORT AND EFFICIENT METHOD FOR THE PREPARATION OF α,p-DIMETHYLSTYRENE FROM CITRAL
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Acid catalysed cyclization of citral to give α,p-dimethyl styrene using chloranil as an oxidizing agent is reported.The important aspect of this transformation is the dehydration of intermediate piperitenol followed by dehydrogenation to furnish the target compound in 80.5percent yield.
- Barton, Derek H. R.,Parekh, Shyamal I.
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p. 3353 - 3362
(2007/10/02)
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- Process for treating 2-ethylhexyl p-methoxycinnamate in the presence of a phenol
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A process for treating 2-ethylhexyl p-methoxycinnamic acid ester is described. The process comprises heating, preferably distilling, the ester in the presence of a phenol to insure that the ester is considered Ames negative.
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