LY-329146

N-[4-[6-羟基-3-[4-[2-(4-吗酚醛)乙氧基]苯甲酰]-1-苯并哧-2-基]苯基]-N-(甲基磺酰)甲烷磺酰胺Chemical Name: N-[4-[6-Hydroxy-3-[4-[2-(4-morpholinyl)ethoxy]benzoyl]-1-benzothien-2-yl]phenyl]-N-(methylsulfonyl)methanesulfonamide
CAS No. 191043-78-4
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:Alkylation of ethyl 4-hydroxybenzoate (I) with 1-(2-chloroethyl)piperidine (II) provided adduct (III).After saponification of the ethyl ester group of (III),the resulting carboxylic acid (IV) was treated with oxalyl chloride to furnish the desired acid chloride (V).

合成路线:Reaction of 4-bromoaniline (VI) with methanesulfonyl chloride afforded the bis sulfonamido derivative (VII).Palladium-catalyzed coupling of (VII) with 6-methoxybenzo[b]thiophene-2-boronic acid (VIII) then provided the 2-aryl benzothiophene (IX).Subsequent Friedel-Crafts acylation of (IX) with acid chloride (V) in the presence of AlCl3 gave rise to ketone (X).The methyl ether group of (X) was finally cleaved by treatment with ethanethiol and AlCl3.