چكيده فارسي :
Alzheimer disease (AD) is a complex neurological affection that is clinically characterized
by loss of memory. Rivastigmine, an acetyl cholinesterase (AChE) inhibitor approved in 2000
for the treatment of AD, bears a carbamate moiety in its structure, which is able to react
covalently with the active site of the enzyme [1,2].
Our process for the straight forward synthesis of enantiomerically pure Rivastigmine
Tartarate, (S)-N-ethyl-N-methyl-3-[-(dimethylamino)ethyl]-phenyl carbamate hydrogen-
(2R,3R)-tartarate withUSP38 has been efficiently carried out under mild reaction condition
with NaOMe as a basic catalyst, that is easy to scale up in industry and suitable for the
manufacture of Rivastigmine in active pharmaceutical ingredient (API) demand.
This process is convenient operation and purification and completes the synthesis of
RivastigmineTartarate in 93% overall yield. The purity of product was characterized by
HPLC analysis.
On the basis of previous studies on a series of benzopyrano[4,3-b]pyrrolecarbamates
asacetyl cholinesterase (AChE) inhibitors, we designed and synthesis a series of
conformationally analogues of Rivastigmine by including the N-ethyl-N-methyl carbamoyl
moiety in different azolic systems.
