Synthesis

A Convergent Synthesis of CGS23305, A Thromboxane Synthase Inhibitor

AT Bach, JA Carlson, PP Giannousis

Index: Bach, Andrew T.; Carlson, John A.; Giannousis, Peter P. Synthesis, 1999 , # 5 p. 769 - 774

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Abstract

Abstract: A convergent synthesis of CGS23305 was discovered. The route to the pyridine aldehyde intermediate 5 was reduced from four to two steps. The pyridine aldehyde was converted to the key pyridine aldehyde ester intermediate 7 via Michael Addition of the N, N- diethylenamine 6 to ethyl acrylate. A Wittig alkenation using the multifunctional moiety 19 completed the carbon skeleton assembly. Hydrogenation and hydrolysis afforded ...