A Convergent Synthesis of CGS23305, A Thromboxane Synthase Inhibitor
作者
Andrew Bach,John A. Carlson,Peter P. Giannousis
出处
期刊:Synthesis [Thieme Medical Publishers (Germany)] 日期:1999-05-01卷期号:1999 (05): 769-774被引量:1
标识
DOI:10.1055/s-1999-3458
摘要
All articles of this category 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 Miachel Addition of the N , N -diethylenamine 6 to ethyl acrylate. A Wittig alkenation using the multifunctional moiety 19 completed the carbons keleteon assembly. Hydrogenation and hydrolysis afforded CGS23305 in 44% overall yield from 14 (6 steps). convergent synthesis - pyridine - aldehydes - thromboxane inhibitor