Diastereoselective Protonation of
Lactam Enolates Derived from
(<i>R</i>)-Phenylglycinol. A Novel Asymmetric
Route to
4-Phenyl-1,2,3,4-tetrahydroisoquinolines
posted on 2000-06-21, 00:00authored byNicolas Philippe, Vincent Levacher, Georges Dupas, Guy Quéguiner, Jean Bourguignon
Highly diastereoselective protonation of chiral lactam enolates of 4-substituted-1,4-dihydroisoquinolin-3-ones is reported. Protonation and
alkylation processes of these lactam enolates derived from phenylglycinol occur with opposite diastereofacial selectivity. This diastereoselective
protonation has been applied to the asymmetric synthesis of (4<i>S</i>)-<i>N</i>-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline <b>9</b> obtained in up to 97% ee.