新产品编号:446633
Chemical Name: 2-Methyl-2(Z)-butenoic acid (3S,3aR,4S,6S,6aR,7S,8S,9bS)-6-acetoxy-4-[3-(4-aminophenyl)-2(E)-propenoyloxy]-3,3a-dihydroxy-7-(octanoyloxy)-2-oxo-3,6,9-trimethyl-2,3,3a,4,5,6,6a,7,8,9b-decahydroazuleno[4,5-b]furan-8-yl ester
CAS No. 216371-66-3
项目整合开发状态: Biological Testing
项目研究机构: Danish University of Pharmaceutical Sci. (Originator), Johns Hopkins University (Originator), University of Copenhagen (Originator)
合成路线:8-O-Debutanoylthapsigargin (II) was obtained by triethylamine-catalyzed methanolysis of thapsigargin (I).Coupling of (II) with N-Boc-4-aminocinnamic acid (III) in the presence of DCC and DMAP provided ester (IV).The Boc protecting group of (IV) was then cleaved by treatment with trifluoroacetic acid.
📌 参考资料/链接：
参考文献标题:Tissue specific prodrug
文献作者:Christensen,S.B.; Issacs,J.T.; Denmeade,S.R.; Lilja,H.(Johns Hopkins University)
参考来源:WO 9852966
📄 详细内容
合成路线:8-O-Debutanoylthapsigargin (II) was obtained by triethylamine-catalyzed methanolysis of thapsigargin (I).Coupling of (II) with N-Boc-4-aminocinnamic acid (III) in the presence of DCC and DMAP provided ester (IV).The Boc protecting group of (IV) was then cleaved by treatment with trifluoroacetic acid.
参考文献标题:Thapsigargin analogues for targeting programmed death of androgen-independent prostate cancer cells
文献作者:Christensen,S.B.; Andersen,A.; Kromann,H.; Treiman,M.; Tombal,B.; Denmeade,S.; Isaacs,J.T.
参考来源:Bioorg Med Chem 1999,7(7),1273