Astrazeneca Ab

Ian Ashworth

Ian Patel

Daniel Levin

A process is described for reacting a vinylogous amide with an &#x3b1;,&#x3b2;-unsaturated ketone in the presence of a silicon compound to form an 1,5-diketone which is converted to a 1,4-dihydropyridine. Asymmetric substituted 1,4-dihydropyridines are synthesized by the process by preparing an asymmetric vinylogous amide by reacting a 1,3-cyclohexanedione with a substantially homo-chiral phenylethylamine. Reaction of the asymmetric vinylogous amide with an &#x3b1;,&#x3b2;-unsaturated ketone in the presence of a silicon compound forms an asymmetric 1,5-diketone. The 1,5-diketone is converted to an asymmetric substituted 1,4-dihydropyridine.

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Stalybridge, United Kingdom

Ian Ashworth