BVT-2733
苯磺酰胺,3-氯-2-甲基-N-[4-[2-(4-甲基-1-哌拉嗪)-2-氧乙基]-2-噻唑基]-,盐酸盐(1:1) 3-氯-2-甲基-N-(4-(2-(4-甲基哌嗪-1-基)-2-氧代乙基)噻唑-2-基)苯磺酰胺 Chemical Name: 3-Chloro-2-methyl-N-[4-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]thiazol-2-yl]benzenesulfonamide hydrochloride
CAS No. 376641-65-5, 376640-41-4 (free base), 376640-42-5 (monotrifluoroacetate)
项目整合开发状态: Preclinical
项目研究机构: Biovitrum (Originator)
合成路线:Acylation of ethyl 2-amino-4-thiazolylacetate (I) with 3-chloro-2-methylbenzenesulfonyl chloride (II) in pyridine affords sulfonamide (III).After alkaline hydrolysis of the ethyl ester group of (III),the resultant carboxylic acid (IV) is coupled to N-methylpiperazine (V) by means of EDC to furnish the target amide.
📌 参考资料/链接：
参考文献标题:Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
文献作者:Emond,R.; Barf,T.; Kurz,G.; Nilsson,M.; Vallgarda,J.(Biovitrum AB)
参考来源:EP 1283831; WO 0190090
📄 详细内容
合成路线:Acylation of ethyl 2-amino-4-thiazolylacetate (I) with 3-chloro-2-methylbenzenesulfonyl chloride (II) in pyridine affords sulfonamide (III).After alkaline hydrolysis of the ethyl ester group of (III),the resultant carboxylic acid (IV) is coupled to N-methylpiperazine (V) by means of EDC to furnish the target amide.
参考文献标题:Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs.Discovery of potent and selective inhibitors of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1
文献作者:Barf,T.; Vallgarda,J.; Emond,R.; Haggstrom,C.; Kurz,G.; Nygren,A.; Larwood,V.; Mosialou,E.; Axelsson,K.; Olsson,R.; Engblom,L.; Edling,N.; Ronquist-Nii,Y.; Ohman,B.; Alberts,P.; Abrahmsen,L.
参考来源:J Med Chem 2002,45(18),3813
产品链接: CAS No. 376641-65-5›› 产品链接: CAS No.376640-41-4››