Method of producing compounds of formula
1
wherein
R
1
is hydrogen or C
1
-C
4
-alkyl;
R
2
is hydrogen, C
1
-C
8
-alkyl, C
3
-C
6
-cycloalkyl, or a radical —N(R
3
)R
4
; or R
2
and R
6
together are —CH
2
—CH
2
—S—;
R
3
and R
4
are hydrogen, C
1
-C
4
-alkyl, C
3
-C
6
-cycloalkyl or a radical —CH
2
B;
R
6
is hydrogen, C
1
-C
8
-alkyl, aryl or benzyl;
or R
3
and R
6
together are —CH
2
—CH
2
—, —CH
2
—CH
2
—CH
2
—, —CH
2
—O—CH
2
—, —CH
2
—S—CH
2
— or —CH
2
—N(R
5
)—CH
2
—;
X is CH—CN; CH—NO
2
or N—NO
2
;
A is an optionally substituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical; and
B is optionally substituted phenyl, 3-pyridyl or thiazolyl;
characterised in that a compound of formula
2
wherein R
2
, R
6
and X have the same significance as given above in formula (I), is reacted in the presence of a phase transfer catalyst and a base with a compound of formula
3
wherein A and R
1
have the same significance as given above in formula (I) and Q is a leaving group.
生产式1化合物的方法,其中R1为氢或C1-C4烷基;R2为氢,C1-C8烷基,C3-C6环烷基或基团—N(R3)R4;或R2和R6一起为—
CH2— —S—;R3和R4为氢,C1-C4烷基,C3-C6环烷基或基团— B;R6为氢,C1-C8烷基,芳基或苄基;或R3和R6一起为— — —,— — — —,— —O— —,— —S— —或— —N(R5)— —;X为CH—CN、CH—
NO2或N— ;A为可选取代的芳香或非芳香、单环或双环杂环基;B为可选取代的苯基,3-
吡啶基或
噻唑基;其特征在于,在相转移催化剂和碱的存在下,一种式2化合物(其中R2、R6和X的意义与式(I)中所给出的相同)与一种式3化合物(其中A和R1的意义与式(I)中所给出的相同,Q为离去基团)反应。