首页> 外国专利> FOERFARANDE FOER AENDRING AV KFFIGURATIONEN AV OPTISKT AKTIVA FOERENINGAR OCH I FOERENINGEN ANVAENOPTISKT AKTIVA MELLANPRODUKTER

FOERFARANDE FOER AENDRING AV KFFIGURATIONEN AV OPTISKT AKTIVA FOERENINGAR OCH I FOERENINGEN ANVAENOPTISKT AKTIVA MELLANPRODUKTER

机译:修改光学有效协会和实际有效中间产品协会的程序

摘要

For the contracting states BE, CH, DE, FR, GB, IT, LI, NL, SE 1. A process for inverting the configuration at the optically active carbon atom (*) in compounds of the formula I see diagramm : EP0102520,P6,F1 in which A represents a cyclopentylphenyl radical and R represents the t-butyl radical, which comprises converting these compounds by formylation into optically active compounds of the formula II see diagramm : EP0102520,P6,F2 in which A and R have the meanings defined above, while maintaining the configuration at the carbon atom (*), converting these compounds, by treatment with a strong acid or an acid halide, into optically active cyclic compounds of the formula III see diagramm : EP0102520,P6,F3 in which A and R have the meanings defined above and in which X**(anion) represents the anion of a strong acid or of a halogen atom, and converting these oxazolinium derivatives (III), by acid or alkaline hydrolysis, if appropriate via the stage of the N-formyl compound, into optically active compounds of the formula IV see diagramm : EP0102520,P7,F4 in which A and R have the meanings defined above, possessing the same structure as the starting material I, but having an opposite configuration at the carbon atom (*). For the contracting state AT 1. A process for inverting the configuration at the optically active carbon atom (*) in compounds of the formula I see diagramm : EP0102520,P7,F1 in which A represents a cyclopentylphenyl radical and R represents the t-butyl radical, which comprises converting these compounds by formylation into optically active compounds of the formula II see diagramm : EP0102520,P7,F2 in which A and R have the meanings defined above, while maintaining the configuration at the carbon atom (*), converting these compounds, by treatment with a strong acid or an acid halide, into optically active cyclic compounds of the formula III see diagramm : EP0102520,P7,F3 in which A and R have the meanings defined above and in which X**(anion) represents the anion of a strong acid or of a halogen atom, and converting these oxazolinium derivatives (III), by acid or alkaline hydrolysis, if appropriate via the stage of the N-formyl compound, into optically active compounds of the formula IV see diagramm : EP0102520,P7,F4 in which A and R have the meanings defined above, possessing the same structure as the starting materail I, but having an opposite configuration at the carbon atom (*).
机译:对于缩合状态BE,CH,DE,FR,GB,IT,LI,NL,SE1。用于反转式I化合物中旋光性碳原子(*)构型的方法,见图:EP0102520,P6 ,F1,其中A代表环戊基苯基基团,R代表叔丁基基团,其包括通过甲酰化将这些化合物转化为式II的光学活性化合物,参见图:EP0102520,P6,F2,其中A和R具有所定义的含义如上,在保持碳原子(*)构型的同时,通过用强酸或酰卤处理将这些化合物转化为式III的光学活性环状化合物,参见图:EP0102520,P6,F3,其中A和R具有上面定义的含义,其中X **(阴离子)代表强酸或卤素原子的阴离子,并且如果合适的话,通过酸或碱水解将这些恶唑啉鎓衍生物(III)转化。 N-甲酰基化合物,整数式IV的光学活性化合物参见图:EP0102520,P7,F4,其中A和R具有以上定义的含义,具有与起始原料I相同的结构,但在碳原子(*)处具有相反的构型。对于收缩态AT 1,使式I化合物中的旋光活性碳原子(*)的构型反转的方法,参见示意图:EP0102520,P7,F1,其中A代表环戊基苯基,R代表叔丁基基团,其包括通过甲酰化将这些化合物转化为式II的旋光活性化合物,参见示意图:EP0102520,P7,F2,其中A和R具有上述定义,同时保持碳原子(*)的构型,将其转化通过用强酸或酰基卤处理,将这些化合物制成式III的旋光环状化合物,参见图:EP0102520,P7,F3,其中A和R具有以上定义的含义,并且其中X **(阴离子)表示强酸或卤素原子的阴离子,然后将这些恶唑啉鎓衍生物(III)通过酸或碱水解(适当时通过N-甲酰基化合物的阶段)转化为t的旋光化合物式IV参见图:EP0102520,P7,F4,其中A和R具有上述定义,具有与起始原料I相同的结构,但在碳原子(*)上具有相反的构型。

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