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ENANTIONSELECTIVE PROCESSES TO INSECTICIDAL 3-ARYL-3-TRIFLUOROMETHYL-SUBSTITUTED PYRROLIDINES

机译:对杀虫剂3-芳基-3-三氟甲基取代的吡咯烷的灭菌方法

摘要

The present invention relates to processes for the enantio-selective preparation of spyrrolidine derivatives useful in the manufacture of pesticidally active compounds, as well as to intermedates in the processes. The processes include those comprising (a-i) reacting a compound of formula (Ia), formula (Ia), wherein P is alkyl, aryl or heteroaryl, each optionally substituted, wherein the heteroaryl is connected at P via a ring carbon atom; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is aryl or heteroaryl, each optionally substituted; with a source of cyanide in the presence a chiral catalyst to give a compound of formula IIa, formula (IIa), wherein P, R1 and R2 are as defined for the compound of formula (Ia); and (a-ii) oxidising the compound of formula IIa with a peroxy acid, or peroxide in the presence of an acid to give a compound of formula (VI), formula (VI), wherein R1 and R2 are as defined for the compound of formula (Ia).
机译:本发明涉及用于制备杂种活性化合物的筛选衍生物的纺吡啶衍生物的方法,以及该方法中的中间体。该方法包括包含式(A-1)的那些,使式(IA)化合物,式(IA),其中P是烷基,芳基或杂芳基,每种任选取代,其中杂芳基通过环形碳原子在P处连接; R 1 是氯二氟甲基或三氟甲基; R 2 是芳基或杂芳基,每种任选取代;在存在手性催化剂中,用氰化物的源源,得到式IIA的化合物,其中P,R 1和R 2 如定义式(IA)的化合物; (A-II)用过氧酸氧化式IIA化合物,或在酸存在下过氧化物,得到式(VI)化合物,式(VI),其中R 1 R 2 与式(IA)化合物定义。

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