Practical Synthesis of a Potent Bradykinin B1 Antagonist via Enantioselective Hydrogenation of a Pyridyl N-Acyl Enamide
Paul D. O’Shea, Danny Gauvreau, Francis Gosselin, Greg Hughes, Christian Nadeau, Amelie Roy and C. Scott ShultzPdf to the paper
So it seems the Merck Lab has a little gift of science for us in the new JOC. The paper's main points were mainly comprised of a Suzuki and some Carbo acid activation, but they also threw in some fun chirality aswell.
In preparing their reagent for the Suzuki they had to induce chirality within it and although got a little steppy had very good yields and came out with product.
After this the ran the Suzuki, deprotected the amine and did the Carbo activation with EDC and HOBT.
Update: I did some more reading in the paper and the Tangphos is actually binding to the Rh catalyst so I thought I'd post the Rh Catalyst aswell.
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