923035-05-6Relevant academic research and scientific papers
PREPARATION METHOD OF RIVASTIGMINE, ITS INTERMEDIATES AND PREPARATION METHOD OF THE INTERMEDIATES
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Page/Page column 8, (2010/10/05)
The present invention provides N-methylethylcarbamino-3-[(S)-1-(methyl-[(S)-1-phenylethyl] amino) ethyl] phenyl ester represented by formula (II) and its preparation method. The present invention also provides (S)-1-(3-methoxyphenyl)-N-methyl-N-[(S)-1-phenylethyl] ethylamine and 3-[(S)-1-(methyl-[(S)-1-phenylethyl] amino) ethyl] phenol as intermediates of the compound represented by formula (II), and the use of the compound represented by formula (II) for preparing rivastigmine used for treating Alzheimer disease.
Novel convenient synthesis of rivastigmine
Hu, Meng,Zhang, Fu-Li,Xie, Mei-Hua
experimental part, p. 1527 - 1533 (2009/10/17)
A novel and convenient synthesis of rivastigmine has been reported. This procedure provides high yield and excellent enantiomeric excess (100% ee) starting from the diastereromerically pure (S)-1-(3-methoxyphenyl)-N-[(S)-1- phenylethyl] ethanamine. Copyright Taylor & Francis Group, LLC.
METHOD OF OBTAINING PHENYL CARBAMATES
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Page/Page column 14, (2008/12/06)
The invention relates to a method of obtaining phenyl carbamates (I), wherein R 1 is lower alkyl C 1 -C 5 or benzyl and R 2 is methyl, ethyl or propyl, consisting in reacting L-(S)-3-[(1-methylamino)ethyl]phenol, in the presence of a base, with a carbamoyl halide in order to obtain an intermediate and, subsequently, subjecting said intermediate to a reducing amination reaction or a methylation reaction by reacting same with a methyl halide. The above-mentioned compounds (I) include rivastigmine, a compound that inhibits cholinesterase in the central nervous system, and can be used in the treatment of neurodegenerative diseases (E.g. senile dementia and Alzheimer's disease).
