申请人:——
公开号:US20020095038A1
公开(公告)日:2002-07-18
A novel method for the synthesis of piperazine and its derivatives of formula 1,
1
wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms;
R
1
is selected from hydrogen, a methyl group, a phenyl group optionally substituted with an alkyl group having 1 to 6 carbon atoms, or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; and
R
2
is selected from hydrogen, or a methyl group, or a fluoromethyl group;
2
comprising the steps:
a. reacting an ester of formula 11 with substituted or unsubstituted ethylenediamine of formula 7 to give 3,4-dehydropiperazine-2-one and its derivatives of formula 12, wherein R, R
1
, R
2
are as defined above and R
6
is a C
1
to C
4
linear or branched alkyl group; and
b. reacting the 3,4-dehydro-piperazine-2-one and its derivatives of formula 12 with a reducing agent to yield the piperazine and its derivatives of formula 1.
一种合成1,1-哌嗪及其衍生物的新方法,其中R选择氢,或者具有1至6个碳原子的低级烷基基团或苯基烷基基团,其烷基具有1至4个碳原子; R1选择氢、甲基、苯基(可选地带有1至6个碳原子的烷基基团)或苯基烷基基团,其烷基具有1至4个碳原子; R2选择氢、甲基或氟甲基; 2包括以下步骤:a. 反应式11的酯与式7的取代或未取代的乙二胺反应,得到式12的3,4-去氢哌嗪-2-酮及其衍生物,其中R,R1,R2如上所定义,R6为C1至C4线性或支链烷基基团; b. 反应式12的3,4-去氢哌嗪-2-酮及其衍生物与还原剂反应,得到式1的哌嗪及其衍生物。