1-烃基-5-取代氨基-4-吡唑(N-取代)甲酰胺的合成及生物活性研究

本文采用吡唑并3,4-d]-1,3-噁嗪-6-酮衍生物(Ⅰ)与伯胺反应,合成了1-烃基-5-取代苯甲酰胺基-4-吡唑(N-取代)甲酰胺(Ⅱ);由LiAlH₄,对Ⅱ分子中2个酰胺基的选择性还原合成了1-烃基-5-取代氨基-4-吡唑(N-取代)甲酰胺(Ⅲ).共合成新化合物23个,通过¹HNMR、¹³CNMR、MS、IR等证明了它们的化学结构,初步生物活性测定表明化合物Ⅱ具有一定的抗癌活性和农药活性。

Studies on the Synthesis and Biological Activity of 1-Alkyl(or Aryl)- 5-Substituted Amino-4-(N-Alkyl carbamoyl)pyrazole

In order to look for biologically active heterocyclic compounds, pyrazolo3,4-d]-1 ,3-oxazin-6-ones(Ⅱ) were reacted with primary amines, l-alkyl(or aryl)-5-benzoylamino-4-(N-alkyl carbamoyDpyrazole (Ⅱ) were obtained.By the reduction of Ⅱ, it was found for the first time that only one of the two amide groups in compound Ⅱ was reduced selectively to give 1-alkyl (or aryl)-5-substituted amino-4-(N-alkyl carbamoyl) pyrazole (Ⅲ).Twenty three new compounds were prepared and identified by ¹H NMR,¹³C NMI,IRand MS.The preliminary biological activities of the products indicate that some of them possess antitumor and pesticidal activities.