- Regioselective synthesis of 2,4,6-triaminopyridines
-
A regioselective synthesis of 2,4,6-trisubstituted pyridine is described starting from 2,6-dibromo-4-nitropyridine. All three different regioisomers of the 2,4,6-triamino substituted pyridine have been synthesized in four to five steps. The method described is a general route to unsymmetrical 2,4,6-trisubstituted amino pyridines.
- Shetty, Rupa,Nguyen, Duyan,Flubacher, Dietmar,Ruggle, Franziska,Schumacher, Andreas,Kelly, Martha,Michelotti, Enrique
-
p. 113 - 117
(2007/10/03)
-
- Synthesis of [4,6-3H]-2-pyridone and [3H]-RS-91309
-
We describe herein, a novel synthesis of the previously unreported compound, 4,6-dibromo-2-pyridone (3) and its use in the preparation of [3H]-RS-91309, a potassium channel modulator. This key intermediate, (3), was reduced with carrier free tritium gas to furnish [4,6-3H]-2-pyridone (9) having a specific activity of 50 Ci/mmole. Condensation of (9) with epoxide (10), followed by elaboration of the resulting chromene methyl group of (12) gave [3H]-RS-91309 (14) whose specific activity was also 50 Ci/mmole. This chemistry, as well as the solution of several microscale related stoichiometry problems is discussed.
- De Keczer,Parnes
-
p. 765 - 772
(2007/10/02)
-