SB-568849
N-(4-(2-(二乙胺基)乙氧基)-3-甲氧基苯基)-N-甲基-4'-(三氟甲基)-[1,1'-双苯]-4-羧酰胺Chemical Name: N-[4-[2-(Diethylamino)ethoxy]-3-methoxyphenyl]-N-methyl-4'-(trifluoromethyl)biphenyl-4-carboxamide
CAS No. 395679-53-5
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:Substitution of 1-chloro-2-methoxy-4-nitrobenzene (I) with 2-(diethylamino)ethanol (II) gives rise to ether (III).Subsequent nitro group reduction in (III) by catalytic hydrogenation affords aniline (IV).Condensation of amine (IV) with triethyl orthoformate,followed by reduction of the resultant formimidate (V) with NaBH4 leads to the N-methyl amine (VI).This is acylated by 4-bromobenzoyl chloride (VII) to furnish the bromobenzamide (VIII).Finally,Suzuki coupling of bromide (VIII) with 4-trifluoromethylphenylboronic acid (IX) produces the title biphenyl compound
📌 参考资料/链接:
参考文献标题:Carboxamide cpds.and their use as antagonists of a human 11CBy receptor
文献作者:Stemp,G.; Johnson,C.N.; Jones,M.; O'Toole,C.A.; Thewlis,K.M.; Witty,D.(GlaxoSmithKline plc)
参考来源:EP 1305304; WO 0210146