【药物名称】
化学结构式(Chemical Structure):
参考文献No.50765
标题:Brefeldin A derivs.
作者:Cushman, M.S.; Devraj, R.; Argade, A.B.; Haughwitz, R.D. (Purdue Research Foundation)
来源:US 6362218; WO 9931084
合成路线图解说明:

Michael addition of 2-mercaptoethanol (II) to the unsaturated lactone function of (+)-brefeldin A (I) in the presence of Proton Sponge afforded the sulfanyl adduct (III). The title sulfoxide was then obtained by oxidation of sulfide (III) with meta-chloroperbenzoic acid.

参考文献No.540953
标题:Design and synthesis of brefeldin A sulfide derivatives as prodrug candidates with enhanced aqueous solubilities
作者:Argade, A.B.; Devraj, R.; Vroman, J.A.; Haugwitz, R.D.; Hollingshead, M.; Cushman, M.
来源:J Med Chem 1998,41(18),3337
合成路线图解说明:

Michael addition of 2-mercaptoethanol (II) to the unsaturated lactone function of (+)-brefeldin A (I) in the presence of Proton Sponge afforded the sulfanyl adduct (III). The title sulfoxide was then obtained by oxidation of sulfide (III) with meta-chloroperbenzoic acid.

参考文献No.630326
标题:Design and synthesis of (+)-brefeldin A sulfide prodrugs with enhanced aqueous solubilities
作者:Fox, B.M.; et al.
来源:222nd ACS Natl Meet (Aug 26 2001, Chicago) 2001,Abst MEDI 97
合成路线图解说明:

Michael addition of 2-mercaptoethanol (II) to the unsaturated lactone function of (+)-brefeldin A (I) in the presence of Proton Sponge afforded the sulfanyl adduct (III). The title sulfoxide was then obtained by oxidation of sulfide (III) with meta-chloroperbenzoic acid.

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