- Preparation method and application of cisatracurium besilate
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The invention provides a preparation method and application of cisatracurium besylate, and the preparation method comprises the following steps: (1) dissolving R-tetrahydropapaverine-N-acetyl-L-leucine salt, adjusting the pH value with an alkaline solution, and then mixing with methyl 3-bromopropionate and alkali for reaction to obtain an intermediate A; (2) mixing and reacting the intermediate A obtained in the step (1) with alkali to obtain an intermediate B; (3) mixing and reacting the intermediate B obtained in the step (2) with a methylation reagent to obtain an intermediate C; and (4) mixing and reacting the intermediate C obtained in the step (3), a catalyst and a dehydrating agent to obtain cisatracurium besylate. The preparation method provided by the invention is safe in production process, high in yield, few in isomer and low in maximum single impurity.
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- PROCESS FOR PRODUCING CISATRACURIUM AND ASSOCIATED INTERMEDIATES
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The present invention provides a process of producing cisatracurium compounds, e.g., cisatracurium besylate, from isoquinolinium salts of the structural formula (VIIA) wherein X- is an anion and R is H or a C1-C6 alkyl, or an activated form of the carboxylic acid with 1,5-pentanediol to form a cisatracurium salt, optionally via an intermediate compound (VIII). The cisatracurium compounds can be purified using simple techniques to afford pure cisatracurium besylate without the need for HPLC purification.
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Page/Page column 17
(2009/03/07)
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- PROCESS FOR PRODUCING CISATRACURIUM COMPOUNDS AND ASSOCIATED INTERMEDIATES
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The present invention provides processes for producing isoquinolinium compounds, and for converting them into cisatracurium salts, e.g., cisatracurium besylate
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Page/Page column 39
(2008/12/08)
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- NOVEL ISOQUINOLINIUM COMPOUNDS USEFUL IN THE PREPARATION OF CISATRACURIUM AND ASSOCIATED INTERMEDIATES
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The present invention provides novel isoquinolinium compounds, methods of producing the isoquinolinium compounds, and methods for converting them into cisatracurium, e.g., cisatracurium besylate. The isoquinolinium compounds of the present invention can be obtained in the form of solids, which can be purified using simple techniques and can be used to afford pure cisatracurium besylate without HPLC purification
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Page/Page column 39
(2008/12/08)
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