申请人:Zierke Thomas
公开号:US20110144336A1
公开(公告)日:2011-06-16
A process for preparing piperazinedione derivatives of the formula I
in which
R
1
is hydrogen, alkyl, alkenyl, alkynyl and alkylcarbonyl,
R
2
is hydrogen, alkyl, alkenyl, C
3
-C
4
-alkynyl and C(═O)R
11
,
R
3
, R
4
are each hydrogen, alkyl and haloalkyl, where the groups may be substituted, which comprises reacting amines of the formula II
H
2
N—R
1
II
in which
R
1
is hydrogen and alkyl which may optionally be substituted with N-acylated amino acid derivatives of the formula III
in which
X is halogen,
Y is halogen, alkoxy or phenyloxy which may be substituted and
R
2
, R
3
and R
4
are each as defined at the outset,
under basic conditions in an aqueous solvent.
制备式I的哌哒二酮衍生物的方法,其中R1是氢、烷基、烯基、炔基和烷基羰基,R2是氢、烷基、烯基、C3-C4-炔基和C(═O)R11,R3、R4均为氢、烷基和卤代烷基,其中基团可能被取代,包括在水溶剂中在碱性条件下将式II的胺-H2N—R1II(其中R1是氢和烷基,可以选择地被取代为N-酰化氨基酸衍生物的式III)与X为卤素、Y为卤素、烷氧基或苯氧基且可能被取代,R2、R3和R4如前所述的在基团进行反应。