Novel methods for site-selective lithiation of 1-(chlorophenyl)pyrroles and 1-(methoxyphenyl)pyrroles are described. Mono- or dilithiations are governed by change of both the temperature and the solvent from tetrahydrofuran to diethyl ether. Regioselectivities could be influenced by the quality of the metallating agent. Thus, 1-(4-chlorophenyl)pyrrole was dilithiated with activated butyllithium at 0 °C to afford a valuable intermediate in a pyrrolobenzoxazepine synthesis.
|Number of pages||5|
|Journal||Journal of the Chemical Society. Perkin Transactions 1|
|Publication status||Published - Jan 1 2001|
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