A concise enantioselective synthesis of (R)-selegiline, (S)-Benzphetamine (cas 156-08-1) and formal synthesis of (R)-sitagliptin via electrophilic azidation of chiral imide enolates

Add time:09/29/2019    Source:infona.pl

A concise and high yielding enantioselective synthesis of (R)-selegiline, an anti-Parkinson’s drug, (S)-benzphetamine, an anti-obesity agent, and (S)-sitagliptin, an anti-diabetic drug has been described starting from commercially available starting materials employing Evans’ electrophilic azidation of chiral imide enolates as a key chiral inducing step, which proceeds in a highly diastereoselective manner (>99%).

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