Synlett

Synthesis of THIQ derivatives as potential boron neutron capture therapy agents: N-functionalized o-carboranylmethyl benzopiperidines

CH Lee, JM Oh, JD Lee, H Nakamura, J Ko, SO Kang

Index: Lee, Chai-Ho; Oh, Jung Mee; Lee, Jong-Dae; Nakamura, Hiroyukiki; Ko, Jaejung; Kang, Sang Ook Synlett, 2006 , # 2 p. 275 - 278

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Citation Number: 3

Abstract

Abstract A method for synthesizing o-carborane substituted tetrahydroisoquinolines containing a polar functional group such as sulfonic or phosphoric acid on the nitrogen atom of the piperidine ring, starting from N-(2-arylethyl) sulfamic acid or 2- arylethylamidophosphate, is described. In vitro studies showed that the desired compounds 7a and 10b accumulate to high levels in B-16 melanoma cells despite low cytotoxicity.