[EN] PROCESS FOR THE RACEMISATION OF ENANTIOMERICALLY ENRICHED ALPHA-AMINO NITRILES<br/>[FR] METHODE DE RACEMISATION D'ALPHA-AMINONITRILES ENRICHIS D'ENANTIOMERES
申请人:DSM IP ASSETS BV
公开号:WO2004046088A1
公开(公告)日:2004-06-03
Process for the racemisation of an enantiomerically enriched α-amino nitrile characterized in that the enantiomerically enriched α-amino nitrile is contacted with a lewis acid catalyst. Preferably an aprotic solvent is used. The lewis acid catalyst preferably comprises a metal chosen from main group elements IA-IVA of the Periodic Table (CAS version), the transition metals and the lanthanides, in particular Al, Ti, Zr, or lanthanides. The catalsyt for example has the general structure MnXpSqLr, and preferably is chosen from the group of aluminum alkoxides, aluminum alkyls, lanthanide alkoxydes and lanthanocenes. The racemisation may be performed in combination with a resolution process, for instance in combination with an enzymatic or a crystallization induced resolution process, preferably in situ, for instance in situ in a crystallization induced asymmetric transformation process.
对富集对映体的α-氨基腈进行消旋的过程特点在于将富集对映体的α-氨基腈与路易斯酸催化剂接触。最好使用无水溶剂。路易斯酸催化剂最好包括从周期表(CAS版本)的主族元素IA-IVA、过渡金属和镧系元素中选择的金属,特别是铝、钛、锆或镧系元素。例如,催化剂具有一般结构MnXpSqLr,最好从铝烷氧化物、铝烷基、镧系烷氧化物和镧系烷基中选择。消旋可以与分离过程结合进行,例如与酶法或结晶诱导的分离过程结合,最好是原位的,例如在结晶诱导的不对称转化过程中原位进行。