申请人：Nett Markus
公开号：US20100184994A1
公开（公告）日：2010-07-22
The present invention relates to a process for preparing 3-difluoromethyl-substituted pyrazole compounds of the formula (I)
in which R
1
is H, halogen, nitro, C
1
-C
8
-alkyl, C
1
-C
8
-haloalkyl, C
3
-C
8
-cycloalkyl, phenyl, naphthyl, hetaryl, cyano, —C(═O)—OR
1a
, —C(═O)—NR
1b
R
1c
, —C(═O)—SR
1d
or —C(═S)—SR
1e
; R
2
is H, C
1
-C
4
-alkyl, benzyl or phenyl; R
3
is H, halogen, C
1
-C
8
-alkoxy, C
1
-C
8
-haloalkoxy, C
3
-C
8
-cycloalkoxy, C
2
-C
8
-alkenyloxy, C
1
-C
8
-alkylthio, C
1
-C
8
-haloalkylthio, C
3
-C
8
-cyclo-alkylthio or C
2
-C
8
-alkenylthio; compounds of the formula (II.a) or (II.b),
in which R
1
and R
3
each have one of the definitions given above; R
4
is halogen, —OR
4a
, —SR
4a
, —O—SO
2
—R
4a
or an —NR
4b
R
4c
group; R
5
and R
6
are each C
1
-C
8
-alkyl, C
1
-C
8
-haloalkyl, C
3
-C
8
-cycloalkyl, benzyl or phenyl, or, together with the nitrogen atom to which they are bonded, are a 3- to 8-membered heterocycle; Lewis acid adducts of compounds of the formula (II.b); the use of compounds of the formula (II.a) or (II.b) and of the Lewis acid adducts for preparing compounds of the formula (I) or (VI);
and to a process for converting such compounds to the corresponding 3-difluoro-pyrazol-4-ylcarboxylic acids.
本发明涉及一种制备3-二氟甲基取代吡唑化合物的方法，其化学式为（I），其中R1为H、卤素、硝基、C1-C8烷基、C1-C8卤代烷基、C3-C8环烷基、苯基、萘基、杂环基、氰基、—C(═O)—OR1a、—C(═O)—NR1bR1c、—C(═O)—SR1d或—C(═S)—SR1e；R2为H、C1-C4烷基、苄基或苯基；R3为H、卤素、C1-C8烷氧基、C1-C8卤代烷氧基、C3-C8环烷氧基、C2-C8烯氧基、C1-C8烷硫基、C1-C8卤代烷硫基、C3-C8环烷硫基或C2-C8烯硫基；化合物的化学式为（II.a）或（II.b），其中R1和R3分别具有上述定义；R4为卤素、—OR4a、—SR4a、—O—SO2—R4a或—NR4bR4c基团；R5和R6分别为C1-C8烷基、C1-C8卤代烷基、C3-C8环烷基、苄基或苯基，或与它们连接的氮原子一起形成3-至8-成员的杂环；化合物的路易斯酸加合物的使用，化合物的化学式为（II.b）；化合物的化学式为（II.a）或（II.b）和路易斯酸加合物的使用，用于制备化合物的化学式为（I）或（VI）；以及将这些化合物转化为相应的3-二氟吡唑-4-羧酸的方法。
