10367-96-1Relevant articles and documents
Preparation method of chloroprocaine hydrochloride
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Paragraph 0034; 0044; 0054; 0064, (2018/02/04)
The invention belongs to the technical field of organic drug synthesis and particularly relates to a preparation method of chloroprocaine. The preparation method includes the steps that 1, 2-chloro-4-nitrobenzoic acid and 2-diethylaminoethanol reaction raw materials are added into a xylene reaction solvent, para-toluenesulfonic acid or immobilized liquid acid or faintly acid metal salt is added to serve as a catalyst, heating is conducted till reflux is achieved, a reaction is carried out for a certain period of time, aftertreatment is carried out, and a water solution of nitrochlor cain is obtained; 2, ammonium chloride and iron powder are added into the water solution of nitrochlor cain, a heating reaction is carried out, aftertreatment is carried out, and crude chloroprocaine hydrochloride is obtained; refining is carried out, and chloroprocaine hydrochloride is obtained. The direct esterification reaction time is short, the production period is shortened by 30% or above, the total yield of the finished product is larger than 30%, and energy consumption is reduced by 25% or above. The content of chloroprocaine hydrochloride is not smaller than 99.0%, the content of related substances is not larger than 1.0%, and the content of a residual solvent (dimethylbenzene) does not exceed 0.1%. The preparation method is suitable for industrial production.
Immobilised Candida antarctica B as efficient catalyst for the synthesis of local anaesthetic intermediates
Giunta, Daniela,Masia, Maria Paola,Marchetti, Mauro,Morrone, Raffaele,Solinas, Maurizio
supporting information, p. 5122 - 5125 (2013/08/28)
We hereby present the development of new reaction conditions for the CALB catalysed esterification of substituted benzoic acids. Using cyclohexane as the reaction media a number of heptyl benzoates have been easily isolated in good to excellent yields (up to 100% at 80 C, 20-24 h). Moreover, the catalytic system has been successfully applied to the synthesis of local anaesthetics intermediates also showing good productivity in recycling experiments.