The invention relates to a preparation method of propiverine hydrochloride; a compound represented by the formula I and 1-methyl-4-piperidinol are subjected to transesterification, and then are subjected to hydrochlorination to generate the product propiverine hydrochloride. The used raw materials and the reaction route are all simple and easy to obtain. More importantly, through scale-up experiment of the route, the yield and purity of the product obtained by the preparation method are found to have little difference from those of a product obtained in laboratories, and the preparation methodis suitable for industrialized popularization.
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Paragraph 0017-0018
(2018/03/25)
SYNTHESIS OF PROPIVERINE HYDROCHLORIDE
The present invention provides a two step esterification process for the synthesis of Propiverine hydrochloride. In the synthetic scheme disclosed herein benzillic acid 1 is directly converted to di-propyl ester ether 7 from the known standard method. The intermediate thus obtained is reacted with N-Methyl 4-hydroxy piperidine in the presence of sodium t-butoxide at room temperature to get Propiverine base 5. This is then finally converted to Propiverine hydrochloride. The process of synthesis provides Propiverine hydrochloride in a very pure form (>99%) with a very good yield. The compound is very useful in treating urinary incontinence.
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Page/Page column 6-7
(2011/10/10)
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