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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 29, Number 2
BKCSDE 29(2)
February 20, 2008 

Preparation of Boronated Heterocyclic Compounds Using Intramolecular Cyclization Reaction
Chai-Ho Lee*, Guo Fan Jin, Hyo-Suk Kim, Hiroyuki Nakamura, Yongseog Chung*, Jong-Dae Lee*
Brain cancer therapy, Boronated heterocyclic compounds, Cytotoxicity
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-arylethyl)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.
357 - 362
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