AWD-12-343
Chemical Name: N-(3,5-Dichloropyridin-4-yl)-2-[5-fluoro-1-(4-fluorobenzyl)-1H-indol-3-yl]-2-oxoacetamide
项目整合开发状态: Preclinical
项目研究机构: Asta Medica (Originator)
合成路线:Alkylation of 5-fluoroindole (I) with 4-fluorobenzyl chloride (II) provided the N-benzyl indole (III).Subsequent reaction of (III) with oxalyl chloride furnished the indolylglyoxylic acid chloride (IV).This was finally coupled with 4-amino-3,5-dichloropyridine (V) to afford the corresponding amide.
📌 参考资料/链接：
参考文献标题:AWD 12-343,a new orally active PDE 4 inhibitor - Synthesis and comparison with SB 207499,rolipram and AWD 12-281
文献作者:H鰂gen,N.; et al.
参考来源:27th Natl Med Chem Symp (June 13 2000,Kansas City) 2000,Abst B-19
📄 详细内容
合成路线:Alkylation of 5-fluoroindole (I) with 4-fluorobenzyl chloride (II) provided the N-benzyl indole (III).Subsequent reaction of (III) with oxalyl chloride furnished the indolylglyoxylic acid chloride (IV).This was finally coupled with 4-amino-3,5-dichloropyridine (V) to afford the corresponding amide.
参考文献标题:AWD 12-343,a new orally active PDE 4 inhibitor - Synthesis and comparison with SB 207499,rolipram and AWD 12-281
文献作者:Egerland,U.; Kronbach,T.; H鰂gen,N.; Poppe,H.; K黶ters,S.; szelenyi,S.
参考来源:16th Int Symp Med Chem (Sept 18 2000,Bologna) 2000,Abst PA-79