FIELD: chemistry.
SUBSTANCE: present invention relates to methods for synthesis of rivastigmine having formula (I), involving reacting 3-(1-dimethylaminoethyl)phenol of formula (V) or its S-enantiomer of formula (V-a) with carbonyl diimidazole, subsequent reaction of the reaction product with ethylmethylamine in an organic solvent to obtain a compound (II) or a compound (I) and optional splitting of the formula (II) compound to obtain a formula (I) compound or carry out a reaction of S-3-(1-dimethylaminoethyl) phenol of formula (V-a) with ethylmethyl carbamoylchloride in an inert organic solvent at high temperature and in the presence of a weak inorganic or organic base.
EFFECT: methods are cheap on an industrial scale and enable use of readily available industrially safe material.
22 cl, 1 dwg, 8 ex
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Authors
Dates
2010-06-27—Published
2005-10-29—Filed