Preparation of boronated heterocyclic compounds using intramolecular cyclization reaction

作者:Lee Chai Ho*; Jin Guo Fan; Kim Hyo Suk; Nakamura Hiroyuki; Chung Yongseog; Lee Jong Dae
来源:Bulletin of the Korean Chemical Society, 2008, 29(2): 357-362.

摘要

A method for synthesizing o-carborane substituted tetrahydroisoquinolines containing a polar functional group such as sulfamide, sulfonic, or phosphoric acid on the nitrogen atom of the piperidine ring, starting from arylethylamine, N-(2-arylethyl)sulfamide, N-(2-aryl ethyl) sulfamic acid or 2-arylethylamidophosphate, is described. In vitro studies showed the desired compounds 10, 15, 19, and 25 synthesized accumulate to high levels in B-16 melanoma cells with low cytotoxicity.

  • 出版日期2008-2-20