- A postoperative or its optical isomers of synthetic and post-processing method
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The invention relates to a synthesis and post-processing method of sulpiride or an optical isomer thereof, and the synthesis and post-processing method include the following steps: under inert gas protection, heating 2-methoxy-5-aminosulfonyl methyl benzoate or 2-methoxy-5-aminosulfonyl ethyl benzoate and 1-ethyl-2-aminomethyl pyrrolidine or an optical isomer thereof at 80-120 DEG C for a plurality of hours, and after the reaction is completed, adding ethanol for processing, cooling, filtering, washing and drying.
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Paragraph 0026; 0027; 0031; 0035
(2018/09/11)
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- Process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)-pyrrolidines by amidation in the presence of lipases
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A process for the enantiomeric resolution of 1-substituted 2-(aminomethyl)pyrrolidines of formula (I) in which R is C1-C6 alkyl, which process comprises the reaction of the racemic amine with benzyl acetate in acetonitrile in the presence of a lipase selected from Pseudomonas cepacia, Pseudomonas fluorescens or Candida rugosa lipases, to give the corresponding 1-substituted N-(pyrrolidin-2-yl-methyl)-acetamides of formula (II), with R configuration, and the residual amine with S configuration, and, if desired, the subsequent hydrolysis of the amide to obtain the amine with R configuration.
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- Synthesis and Inhibitory Activity on Carbonic Anhydrase of Some New Sulpiride Analogues Studied by Means of a New Method
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The pharmacological activity of several new sulpiride analogues was studied by means of a new approach, based on a potentiometric technique with a pCO2 sensor, capable of detecting carbonic anhydrase inhibition at equilibrium conditions.This procedure gives results stated as percent of inhibition of enzymatic activity (IP, inhibitory power).To prove the reliability of the proposed approach and to study structure-activity relationships, several new molecules were synthesized and tested in comparison with the two sulpiride enantiomers.A possible inhibition mechanism is discussed in terms of experimental evidence obtained from the interactions between the molecular structures of the new synthesized compounds and carbonic anhydrase.
- Botre, Claudio,Botre, Francesco,Jommi, Giancarlo,Signorini, Roberto
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p. 1814 - 1820
(2007/10/02)
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