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    • 8. 发明授权
    • Method for the preparation of piperazine and its derivatives
    • 哌嗪及其衍生物的制备方法
    • US06603003B2
    • 2003-08-05
    • US10037309
    • 2001-10-25
    • Sonny SebastianHetal Virendra PatelRajamannar Thennati
    • Sonny SebastianHetal Virendra PatelRajamannar Thennati
    • C07D24104
    • C07D295/023C07D241/04C07D471/14
    • A novel method for the synthesis of piperazine and its derivatives of formula 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; R1 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 R2 is selected from hydrogen, or a methyl group, or a fluoromethyl group; 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, R1, R2 are as defined above and R6 is a C1 to C4 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.
    • 合成哌嗪及其衍生物的新颖方法,其中R选自氢或具有1至6个碳原子的低级烷基或苯基烷基,其烷基具有1至4个碳原子; R 1为 选自氢,甲基,任选被具有1至6个碳原子的烷基取代的苯基,或其烷基具有1至4个碳原子的苯基烷基; 和R 2选自氢或甲基或氟甲基;所述方法包括以下步骤:a。 使式11的酯与取代或未取代的式7的乙二胺反应,得到3,4-脱水哌嗪-2-酮及其式12的衍生物,其中R,R 1,R 2如上所定义,R 6是C 1至C 4直链 或支链烷基; 安布 使3,4-脱氢 - 哌嗪-2-酮及其式12的衍生物与还原剂反应,得到哌嗪及其式1的衍生物。