The invention relates to a method for producing 4-haloalkylnicotinamides having the formula (I):
wherein R
1
is (C
1
-C
4
)haloalky, comprising subjecting one or more 3-((C
1
-C
4
)haloalkyl-3-oxo-1-alkenylamino)nitriles of the formula (II), (III) or (IV):
R
1
—C(O)—CH═CH—NH—CH═CH—CN (II)
R
1
—C(O)—CH═CH—NH—CH(ZR
2
)—CH
2
—CN (III)
R
1
—C(O)—CH═CH—NH—CH(Hal)-CH
2
—CN (IV)
where R
1
is as defined above, R
2
is the same or different and is (C
1
-C
6
)-alkyl and Z is the same or different and is O, S or NR
1
, to a ring-closing reaction and simultaneous hydrolysis in the presence of a strong acid.
本发明涉及一种制备式(I)的4-卤代烷基烟酰胺的方法,其中R1为(C1-C4)卤代烷基,包括将一个或多个式(II)、(III)或(IV)的3-((C1-C4)卤代烷基-3-氧代-1-烯基
氨基)腈置于强酸存在下进行环合反应和同时
水解,其中R1如上所定义,R2相同或不同且为(C1-C6)烷基,Z相同或不同且为O、S或NR1:R1—C(O)—CH═CH—NH—CH═CH—CN(II);R1—C(O)—CH═CH—NH—CH(ZR2)—
CH2—CN(III);R1—C(O)—CH═CH—NH—CH(Hal)- —CN(IV)。