Novel Antagonists of Platelet-Activating Factor. 2. Synthesis and Structure-Activity Relationships of Potent and Long-Acting Heterofused [1, 5] Benzodiazepine and [1, …

…, K Cooper, MJ Parry, MH Stefaniak

Index: Fray, M. Jonathan; Bull, David J.; Cooper, Kelvin; Parry, M. John; Stefaniak, Mark H. Journal of Medicinal Chemistry, 1995 , vol. 38, # 18 p. 3524 - 3535

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Citation Number: 30

Abstract

X= 4-(2-methylimidazo [4, 5-clpyrid-l-yl) phenyl. For definitions of Rz-R4, see Table 7. Method A: diaminopyridine, toluene, reflux. Method B: NaH, CH31, DMF, 20" C. tautomer. A more detailed study of compound 10 revealed that in acidic solution it exists entirely as the enamine tautomer, presumably as the dication 10b (see Figure l), as evidenced by the proton NMR spectrum. A dimesylate salt of 10 can be formed, which is a stable, water- ...