新产品编号:930725

Chemical Name: (+)-cis-2-(2-Adamantyl)-4-(3,4-dimethoxyphenyl)-1,2,4a,5,8,8a-hexahydrophthalazin-1-one
CAS No. 415927-51-4, 415927-52-5 (enantiomer), 415927-50-3 (racemate)
项目整合开发状态: Preclinical
项目研究机构: Altana Pharma (Originator)
合成路线:Resolution of racemic cis-ketoacid (I) by precipitation with (R)-(+)-alpha-methylbenzylamine (II) in EtOH,followed by recrystallization of the corresponding salt from EtOH and final acidic treatment,allows isolation of (+)-ketoacid (IV).Finally,cyclization of (IV) with 2-adamantylhydrazine (V) gives rise to the title phthalazinone.
📌 参考资料/链接:
参考文献标题:Novel selective phosphodiesterase (PDE4) inhibitors.4.Resolution,absolute configuration,and PDE4 inhibitory activity of cis- tetra- and cis-hexahydrophthalazinones
文献作者:Van der Mey,M.; Boss,H.; Couwenberg,D.; Hatzelmann,A.; Sterk,G.J.; Goubitz,K.; Schenk,H.; Timmerman,H.
参考来源:J Med Chem 2002,45(12),2526