98626-61-0Relevant academic research and scientific papers
Industrial preparation method of ropivacaine hydrochloride monohydrate
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Paragraph 0013; 0038; 0041-0042; 0050; 0053-0054, (2021/07/14)
The invention discloses an industrial synthesis method of ropivacaine hydrochloride monohydrate. The method comprises the following steps: dissolving racemized 2-piperidinecarboxylic acid serving as a starting material in an organic solvent, and carrying out alkylation reaction, transesterification, chiral resolution and salification refining to obtain a target product. The raw materials are cheap and easy to obtain, a one-pot method is adopted, organic reagents are easy to recycle and reuse, the reaction safety coefficient is high, the technological operation is simple, few three wastes are generated, and the obtained ropivacaine hydrochloride monohydrate is high in yield and high in purity.
Synthesis of Mepivacaine and Its Analogues by a Continuous-Flow Tandem Hydrogenation/Reductive Amination Strategy
Suveges, Nícolas S.,de Souza, Rodrigo O. M. A.,Gutmann, Bernhard,Kappe, C. Oliver
, p. 6511 - 6517 (2017/12/02)
Herein we report a convenient, fast, and high-yielding method for the generation of the racemic amide anaesthetics mepivacaine, ropivacaine, and bupivacaine. Coupling of α-picolinic acid and 2,6-xylidine under sealed-vessel microwave conditions generates the intermediate amide after a reaction time of only 5 min at 150 °C. Subsequent reaction in a continuous-flow high-pressure hydrogenator (H-Cube ProTM) in the presence of the respective aldehyde directly converts the intermediate to the final amide anaesthetics in a continuous, integrated, multi-step ring-hydrogenation/reductive amination protocol. Merits and limitations of the protocol are discussed.
A process for the preparation of ropivacaine hydrochloride
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, (2017/02/24)
The invention provides a method for preparing hydrochloric acid ropivacaine. Part of parameters and conditions in the prior art are improved, and optimization is performed through the following steps that intermediate (I) separation pH and separation extracting solvent are selected; a catalyst and the usage quantity of the catalyst in a resolution agent are selected; refining solvent is selected. In this way, the yield and purity of the prepared hydrochloric acid ropivacaine are high, the purity reaches up to over 99% under the optimal condition, the percentage of dextrorotary isomer is reduced below 0.5%, standard requirements are completely met, and the hydrochloric acid ropivacaine is suitable for industrial production.
Recycling of pipecoloxylidide via racemization
Thalén, Lisa K.,Hedberg, Martin H.,B?ckvall, Jan-E.
body text, p. 6802 - 6805 (2011/03/18)
A method for the racemization of pipecoloxylidide with a ruthenium catalyst has been developed. This racemization method can be implemented in an integrated process that combines the separation of two enantiomers with racemization of the undesired enantio
