Antiplatelet activity of synthetic pyrrolo-benzylisoquinolines
摘要:
Pyrrolo-benzylisoquinolines were prepared as target compounds and their antiplatelet aggregation activity, adrenoreceptor affinity, and cytotoxicity were screened. Compounds 1d-9d showed specific antiplatelet aggregation activity induced by arachidonic acid and collagen. Among them, 8d and 9d exhibited better activity than the reference drug, aspirin and 9d also showed inhibition of platelet aggregation by all four inducers. (C) 2003 Elsevier Science Ltd. All rights reserved.
Treatment of 1-(2-bromoarylmethyl)-3,4-dihydroisoquinolines with oxalyl chloride and triethylamine gave 1-(2-bromophenyl)-5,6-dihydropyrrolo[2,1-a]isoquinoline-2,3-dione derivatives, for example, 1-(2-bromophenyl)-5,6-dihydro-8,9-dimethoxypyrrolo[2,1-a]isoquinoline-2,3-dione. Radical cyclisation of these derivatives with tributyltin hydride and 1,1-azobis(cyclohexanecarbonitrile) afforded telisatin
用草酰氯和三乙胺处理 1-(2-溴芳甲基)-3,4-二氢异喹啉,得到 1-(2-溴苯基)-5,6-二氢吡咯并[2,1-a]异喹啉-2,3-二酮衍生物,例如,1-(2-溴苯基)-5,6-二氢-8,9-二甲氧基吡咯并[2,1-a]异喹啉-2,3-二酮。这些衍生物与三丁基氢化锡和 1,1-偶氮双(环己烷甲腈)的自由基环化得到 telisatin A、telisatin B 和 lettowianthine。
A Facile Synthesis of Telisatin A via Microwave-Promoted Annulation and Reformatsky Reaction
A facile one-pot synthesis of 2,3-dioxopyrrolo[2,1- A]isoquinolines is reported involving the ringformation of aryl pyruvate derivatives with 3,4-dihydroisoquinolines under basic conditions and utilizing the Reformatsky reaction. Using microwave irradiation, the required compounds were obtained in moderate to good yields.