申请人:BASF SE
公开号:US10961213B2
公开(公告)日:2021-03-30
The present invention relates to a process for preparing benzylic amides of formula I
wherein the variables have the meaning as defined in the description, by reductive amidation of a nitrile of formula II
wherein the variables have the meanings given for formula I, with an activated carbonyl compound of formula III,
and which nitrile is obtained by reaction of a compound of formula IV
with a halogen compound of formula V,
wherein X is a halogen atom, preferably bromo, which halogen compound V in turn is obtained by Sandmeyer reaction of an aniline derivative of formula VI
novel compounds of formula I, and processes for preparing compounds of formula XII
wherein the variables have the meaning as defined in the description by condensing compounds of formula I with compounds of formula X
and subjecting the resulting α,β-unsaturated ketone of formula XI
to a reaction with hydroxylamine to yield compounds of formula XII.
本发明涉及一种制备式 I 苄基酰胺的工艺
式 II 的腈的还原酰胺化反应制备式 I 的苄基酰胺的工艺,其中变量的含义如描述中所定义
其中各变量的含义与式 I 相同,并含有式 III 的活化羰基化合物、
而其中的腈是由式 IV 的化合物反应得到的
与式 V 的卤素化合物、
其中 X 是卤素原子,最好是溴原子,而卤素化合物 V 又是通过式 VI 的苯胺衍生物的桑德迈尔反应得到的
新颖的式 I 化合物和制备式 XII 化合物的工艺
其中变量的含义与描述中通过将式 I 化合物与式 X 化合物缩合而定义的含义相同
并将得到的式 XI 的 α、β-不饱和酮
与羟胺反应,生成式 XII 的化合物。