Pharmaceuticals physostigmine

Organocatalytic asymmetric alkylation methodology has also been efficiently applied in a practical multi-gram synthesis of pharmaceutically interesting, optically active (—)-physostigmine analogs [7]. In the presence of 15 mol% of the catalyst 13 alkylation of the oxindole substrate 12 with chloroacetonitrile furnished the desired product 14 in 83% yield and 73% ee (Scheme 3.3, Eq. 2). The counter-ion of the... 

Tymes07 reported a collaborative study of the analysis of physostigmine in pharmaceutical preparations using octadecyl stationary phases with the mobile phase acetonitrile - 0.05 M... 

Kneczke analyzed pharmaceutical preparations containing pilocarpine and physostigmine as well as their degradation products and preservatives on an octadecyl column using ion-pair... 

Fig. 8.7. HPLC analysis pilocarpine, physostigmine, its degradation products and preservatives in pharmaceutical preparations4 ...

Entrapment of drug substances in liposomes and micelles can lead to changes in their stability. When entrapment reduces the degradation rate, it can be used as a method for stabilizing pharmaceuticals. Aspirin can be partially stabilized by incorporation in L-a-dimyristoylphosphatidylcholine (DMPC)-based liposomes.489-491 Anesthetics such as procaine are also stabilized by incorporation in liposomes.490 Physostigmine salicylate in a phospholipid emulsion is stabilized through interaction with phospholipids at the oil-water interface and through incorporation into the internal phase of the emulsion (Fig. 131).549... 

Despite the fact that physostigmine is an important pharmaceutical, no reports have appeared on efforts to produce this alkaloid by means of plant cell cultures. Daoust (737) reported the fermentative production of physostigmine by means of the microorganism Streptomyces griseofuscus. Iwasa et al. (738) employed Streptomyces pseudogriseo-lus for the production of physostigmine. Murao and Hayashi (739) isolated physostigmine and its N-8 nor derivative from Streptomyces sp. AH-4. 

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