A novel approach to 3-iodothiophenes by direct iodocyclization of alkynylthiol derivatives is presented. A variety of 1-mercapto-3-yn-2-ols 5 (readily available from alkynylation of the corresponding alpha-mercapto aldehydes or alpha-mercapto ketones) were smoothly converted into the corresponding 3-iodothiophene derivatives 6 in good yields by reaction with molecular iodine in the presence of NaHCO3 at room temperature in MeCN as the solvent.
An iodocyclization approach to substituted 3-iodothiophenes
GABRIELE, Bartolo;MANCUSO R;
2012-01-01
Abstract
A novel approach to 3-iodothiophenes by direct iodocyclization of alkynylthiol derivatives is presented. A variety of 1-mercapto-3-yn-2-ols 5 (readily available from alkynylation of the corresponding alpha-mercapto aldehydes or alpha-mercapto ketones) were smoothly converted into the corresponding 3-iodothiophene derivatives 6 in good yields by reaction with molecular iodine in the presence of NaHCO3 at room temperature in MeCN as the solvent.File in questo prodotto:
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