Study On The Synthesis And Biological Activity Of Analogues Of SDB-Ethylenediamine

The thesis works mainly on SDB-ethylenediamine derivatives. Three kinds of close analogues of SDB-ethylenediamine were designed and synthesized. Twenty-five new compounds including nineteen target compounds and six related compounds were prepared through different routes and their structures were confirmed by spectral analyses. Twelve target compounds were tested preliminarily their in vitro anti-tumor activity on L1210 and CHO cells. The cytotoxicity of resulted analogues were increased while the synergism with vincristine were not obvious compared to SDB-ethylenediamine.Chapter 1 IntroductionA brief introduction is made on the background and prospect of both SDB-ethylenedi- amine and close analogues, and the recent study on solanesyl derivatives.Chapter 2 The Synthesis and Biological Activity of the Tertiary Amine Kind of SDB- ethylenediamineThe synthetic route started from aromatic aldehydes (4a, 4b), which was condensed with ethylene diamine to form the corresponding Schiff bases (5a, 5b) that were reduced directly without purification to afford the diamines (6a, 6b) in an one pot reaction. Trisubstituated diamines (7, 9) were prepared from 5 using DMS or related halides by the conventional method to give 7 and 8, then 8 reacted with 2 to form 9.Chapter 3 The Synthesis of the Primary Amine Kind of SDB- ethylenediamineEthylenediamine(1) was reacted with BOC2O to give 2, then p-methoxybezalde-...