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PROCESS FOR RESOLVING OPTIONALLY SUBSTITUTED MANDELIC ACIDS BY SALT FORMATION WITH A CHIRAL BASE CYCLIC AMIDE

机译:通过手性碱式环酰胺盐形成选择性取代的扁桃酸的方法

摘要

The present invention relates to a new process for the resolution of mandelic acid derivatives from racemic mandelic acid derivative mixtures by salt formation with chiral base cyclic amides; to the resolved mandelic acid cyclic amide salts (see, for example, formula (IIa), as well as certain other metal and amine salts of the mandelic acid derivatives, and to the use of the resolved mandelic acid derivatives as intermediates suitable for large-scale manufacturing of, for example, pharmaceutical compounds; Formula (IIa), wherein R is selected from CHF2, H, C1-6 Alkyl, CH2F, CHCl2 and CClF2; and wherein n is 0, 1 or 2; R1 is H or C1-6 Alkyl and X is H, halo or C1-6 Alkyl.
机译:本发明涉及通过与手性碱环酰胺成盐从外消旋扁桃酸衍生物混合物中分离出扁桃酸衍生物的新方法。分辨的扁桃酸环状酰胺盐(例如,式(IIa),以及扁桃酸衍生物的某些其他金属盐和胺盐),以及分辨的扁桃酸衍生物作为适合于大规模生产例如药物化合物;式(IIa),其中R选自CHF2,H,C1-6烷基,CH2F,CHCl2和CClF2;并且其中n为0、1或2; R1为H或C1 -6烷基,X是H,卤素或C1-6烷基。

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