- Preparation method of cisatracurium besilate intermediate R, R'-cis-ester
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The invention discloses a preparation method of cisatracurium besilate intermediate R, R'-cis-ester. The stereoconfiguration of the R, R'-cis-ester is consistent with that of a target product cisatracurium besilate, main process impurities and degradation products are basically consistent with research impurities of a target product cisatracurium besilate, a perfect quality control method is established and comprises the steps that diastereoisomers and S-isomers are controlled, the problems of chiral center formation and chiral conversion do not exist in the subsequent production process, splitting is not needed, the content of the isomers in the finished product is controlled from the source, and the chirality of the final product cisatracurium besilate is guaranteed; and when the base poison material methyl benzenesulfonate is moved forwards to the synthesis of R, R'-cis-ester, so that the residual risk in the target product is greatly reduced, and the clinical use is safer and morereliable.
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Paragraph 0035; 0039-0043; 0044; 0048-0052
(2020/05/08)
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- CISATRACURIUM DERIVATIVES, PREPARATION AND USES THEREOF
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The present invention provides compounds which are useful, e.g., as reference markers for analyzing the purity of cisatracurium and salts thereof, a test method for determining the said purity and processes for preparing reference markers.
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Page/Page column 18; 19
(2009/12/05)
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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 34-36
(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 34-36
(2008/12/08)
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