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
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
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
wherein R1 and R2 are as defined for the compound of formula Ia.
本发明涉及对映体选择性制备用于生产杀虫活性化合物的
吡咯烷衍
生物的工艺,以及工艺中的中间体。这些工艺包括
(a-i) 使式 Ia 的化合物反应
其中
P 是烷基、芳基或杂芳基,各自任选被取代,其中杂芳基通过环碳原子在 P 处连接;
R1 是
氯二
氟甲基或三
氟甲基;
R2 是芳基或杂芳基,各自任选被取代;
在手性催化剂存在下,与
氰化源反应,得到式 IIa 的化合物
其中 P、R1 和 R2 如式 Ia 化合物所定义;和
(a-ii) 在酸存在下,用过氧酸或过氧化物氧化式 IIa 化合物,得到式 VI 化合物
其中 R1 和 R2 如式 Ia 化合物所定义。