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An Efficient Synthesis of Racemic Tolterodine | Korea …

An Efficient Synthesis of Racemic Tolterodine - Tolterodine ; Racemate

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API SYNTHESIS INTERNATIONAL: TOLTERODINE


Manufacturing aspects of R-Tolerodine L-tartrate are presented. Initially, five routes are selected for the synthesis of the product but later based on the criteria related to number of steps, cost of reagents, total time required, environmental conditions, purification methods and yield it is found that two of the routes are the most suitable to obtain Tolterodine. Hence, a re-evaluation is made over these two routes in terms of process complexity as an additional criterion which helps select one route as the most feasible one in terms of scale-up in manufacturing process development for R-Tolterodine Ltartrate. The report also explores on the unit operations required to develop the process in which the choice of equipments are made on the basis of cost, efficiency and possible hazards. The entire unit operations and equipments are presented in a form of process flow diagram clearly indicating the reagents, equipments, product, by-products, wastes and the way they are handled in context to the safety issues related to them. The process chemistry is analysed with detailed manifestations on the reaction types, kinetics and thermodynamics giving emphasis on risk assessment and challenges on scaling up the processes. Finally, a thorough discussion is made highlighting the matters regarding the formulation of R-Tolterodine L-tartrate into tablets and capsules.

Synthesis and Formulation of (R)-Tolterodine-L ..

The configuration of the crucial stereocenter was preserved during the synthesis and the obtained product was identified by chiral HPLC to be the (R)‐tolterodine enantiomer.

SHORT SYNTHESIS OF TOLTERODINE, INTERMEDIATES …

The synthesis of tolterodine and its utility ..

The configuration of the crucial stereocenter was preserved during the synthesis and the obtained product was identified by chiral HPLC to be the (R)‐tolterodine enantiomer.">

Most common amine protection methods

Improved one-pot synthesis of N, N-diisopropyl-3-(2-Hydroxy-5-methylphenyl)-3-phenyl propanamide; a key intermediate for the preparation of racemic Tolterodine

Enantioselective Synthesis of (S)- and (R)-Tolterodine (I) by Asymmetric Hydrogenation of a Coumarin Derivative Obtained by a Heck Reaction.
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