- Purification method of carafine intermediate
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To 3 - hydroxyacetophenone as a raw material, the intermediate 3 - [1 - (dimethylamino) ethyl] phenol is formed by reaction with dimethylamine, and the intermediate is subjected to resolution and purification by a specific resolution system to obtain S - 3 - [1 - (dimethylamino) ethyl] phenol. Compared with the preparation method of the intermediate prepared by the method, the preparation method has the advantages of low cost, high yield, good effect, less environmental pollution, reduced residue of inorganic salt, and favorability for large-scale industrial production.
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Paragraph 0021
(2021/10/02)
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- An Alumino-Mannich Reaction of Organoaluminum Reagents, Silylated Amines, and Aldehydes
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A multi-component coupling using organoaluminum reagents, silylated amines, and aldehydes results in the formation of tertiary amines. Both alkenyl- and alkylaluminum reagents undergo reaction with iminium ion substrates for which the corresponding Petasis borono-Mannich reactions are unsuccessful.
- Tarasewicz, Anika,Ensan, Deeba,Batey, Robert A.
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supporting information
p. 6071 - 6074
(2018/04/27)
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- A 3 - [1 - (dimethylamino) ethyl] phenol preparation method
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The invention provides a method for preparing 3-[1-(dimethylamino)ethyl]phenol II. According to the method, by the following reaction formula shown in the description, 3-[1-(methylamino)ethyl)phenol III is prepared from meta-hydroxyl acetophenone IV, which serves as a raw material, through leuckart reaction and is subjected to eschweiler-clarke reaction so as to obtain 3-[1-(dimethylamino)ethyl]phenol II. The method provided by the invention has the advantages that the synthesis route is short, the raw material is cheap and easily available, hazardous and noxious substances are not required to be used, the operation is easy, the production cost is low, and the problems such as complicated reaction operation, high cost, low yield and the like in the prior art are solved. The method is applicable to industrial production and has a relatively high application value.
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Paragraph 0041-0046; 0051-0053; 0063-0071
(2017/09/01)
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- 2,4-bis-substituted acetophenone compound, optical isomers and pharmaceutically acceptable salts thereof and application of 2,4-bis-substituted acetophenone compound and optical isomers and pharmaceutically acceptable salts thereof
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The invention relates to a 2,4-bis-substituted acetophenone compound and optical isomers and pharmaceutically acceptable salts thereof. The invention further discloses an application of the 2,4-bis-substituted acetophenone compound and the optical isomers and pharmaceutically acceptable salts thereof in the aspect of treatment of neural degeneration diseases. The novel compounds have acetylcholinesterase inhibition activity and A beta aggregation inhibiting ability, and hydrolyzates of the novel compounds further have a metal ion chelation action, so that the novel compounds can be used for carrying out treatment from a plurality of targets and have a better application prospect in the treatment of the neural degeneration diseases.
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- 1 -(DIMETHYLAMINO)ETHYL-SUBSTITUTED 6H-BENZO[C]CHROMEN-6-ONES AGAINST SENILE DEMENTIA
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This invention relates to novel (±)1-(Dimethylamino)ethyl substituted 6H-benzo[c]chromen-6-one compounds which are useful as pharmaceutical compositions.
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Page/Page column 8; 9
(2014/09/03)
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- Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors
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Hydroxylated 6H-benzo[c]chromen-6-one derivatives (i.e., urolithins) are the main bioavailable metabolites, and biomarkers of ellagitannins present in various nutrition. Although these dietaries, the sources of urolithins, are employed in folk medicine as cognitive enhancer in the treatment of Alzheimer's Disease, urolithins have negligible potential to inhibit acetylcholinesterase and butyrylcholinesterase enzymes, the validated targets of Alzheimer's Disease. Therefore, within this research, a series of 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives has been designed, synthesized, and their biological activities were evaluated as potential acetylcholinesterase and butyrylcholinesterase inhibitors. The compounds synthesized exerted comparable activity in comparison to rivastigmine, galantamine, and donepezil both in in vitro and in vivo studies.
- Gulcan, Hayrettin Ozan,Unlu, Serdar,Esiringu, Ilker,Ercetin, Tugba,Sahin, Yasemin,Oz, Demet,Sahin, Mustafa Fethi
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p. 5141 - 5154
(2015/02/19)
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- Amorphous and crystalline forms of rivastigmine hydrogentartrate
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Rivastigmine hydrogentartrate in amorphous form or in a crystalline form characterized by an X-ray powder diffraction pattern exhibiting peaks at 2Θ values of 5.1, 14.7, 16.5, 17.6, 18.6, 20.4, 21.1° ± 0.2° (Form I), or 2Θ values of 9.5, 11.3, 13.2, 14.1, 15.5, 19.1 20.0° ± 0.2° (Form II), methods for its preparation and pharmaceutical compositions comprising the same.
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Page/Page column 11
(2008/12/06)
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- IMPROVED PROCESS FOR THE PREPARATION OF RIVASTIGMINE
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The present invention relates to an improved process for preparation of Rivastigmine of formula (I) or pharmaceutically acceptable salts thereof comprising a step of N-methylation of compound of formula (III), wherein R1 = R2 = H or R1 = H and R2 = CH3 or an acid addition salt thereof, using paraformaldehyde in the presence of Raney Nickel and hydrogen in a suitable solvent to obtain compound of formula (II).
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Page/Page column 7
(2008/06/13)
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- Process for the preparation of Rivastigmine
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The present invention relates to an improved process for preparation of Rivastigmine of formula (I) or pharmaceutically acceptable salts thereof comprising a step of N-methylation of compound of formula (III), wherein R1=R2=H or R1=H and R2=CH3 or an acid addition salt thereof, using paraformaldehyde in the presence of Raney Nickel and hydrogen in a suitable solvent to obtain compound of formula (II).
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Page/Page column 4
(2010/11/30)
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- AN EFFICIENT METHOD FOR PREPARATION OF (S)-3-[(1-DIMETHYL AMINO)ETHYL]-PHENYL-N-ETHYL-N-METHYL-CARBAMATE
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The present invention relates to a method for preparation of substituted phenyl carbamate and pharmaceutically acceptable salts thereof, which are of current pharmaceutical interest. The substituted phenyl carbamate and pharmaceutically acceptable salts thereof are useful to raise cholinergic activity in the central nervous system and useful in treatment of diseases such as Alzheimer's disease, Down's syndrome, Huntingdon's chorea, Friedrich's ataxia etc. (S)-3-[(1-dimethyl amino)ethyl]- phenyl-N-ethyl-N-methyl-carbamate (I) is the active ingredient of the pharmaceutical composition referred in US 5,602,176. This compound is also used to induce selective inhibition of acetylcholinesterase activity in the brain.
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Page/Page column 4; 11
(2010/11/30)
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- Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors
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A series of 2-phenoxy-indan-1-one derivatives have been designed, synthesized, and tested as acetylcholinesterase inhibitors. The most potent compound exhibited high AChE inhibitory activity (IC50 = 50 nM), and the molecular docking study indicated that it was nicely accommodated by AChE.
- Sheng, Rong,Lin, Xiao,Li, Jingya,Jiang, Yanke,Shang, Zhicai,Hu, Yongzhou
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p. 3834 - 3837
(2007/10/03)
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- A METHOD OF PRODUCTION OF (-)-(S)-3-[1-(DIMETHYLAMINO)ETHYL]PHENYL-N-ETHYL-N-METHYLCARBAMATE
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The compound of formula (III), optionally its alkaline salt, is reacted with a compound of formula VII, wherein X is a leaving group, resulting in (S)-rivastigmine of formula II, which is then optionally converted into (S)-rivastigmine hydrogentartrade of formula I.
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- A PROCESS FOR THE PREPARATION OF PHENYLCARBAMATES
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A process for the preparation of compound of formula (I); wherein R is hydrogen, linear, branched or cyclic lower alkyl, cyclohexyl, allyl, propargyl or benzyl; R is hydrogen, methyl, ethyl or propyl; or R and R together with the nitrogen to which they are attached form a cyclic moiety of three to eight-membered ring, with or without a hetero atom like nitrogen or oxygen; R is hydrogen or lower alkyl; R and R are the same or different and each is a lower alkyl; comprising reacting compound of formula (II); wherein R, R and R are as defined above, with compound of formula (III); wherein Rand R are as defined above, in the presence of a base, and further resolving the compound of formula (I) to obtain (S)-isomer of compound of formula (I), substantially free of R-isomer.
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