tRA-96023, SB-RA-31012

Chemical Name: [2aR-(2aalpha,4beta,4abeta,6beta,9alpha,11beta,12alpha,12aalpha,12balpha)]-6,9,12b-Triacetoxy-12-benzoyloxy-4-[3-(4-benzoylphenyl)-2(E)-propenoyloxy]-11-hydroxy-4a,8,13,13-tetramethyl-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3
项目整合开发状态: Preclinical
项目研究机构: Roswell Park Memorial Inst. (Originator), State University of New York,Stony Brook (Originator)
合成路线:The compound was prepared by esterification of the 7-hydroxyl group of 13-acetylbaccatin III (I) with 4-benzoylcinnamoyl chloride (II) in the presence of 4-dimethylaminopyridine in CH2Cl2.

合成路线:Palladium-catalyzed coupling of 4-bromobenzophenone (I) with methyl acrylate (II) afforded 4-benzoylcinnamic ester (III),which was hydrolyzed to acid (IV) with NaOH.Condensation with taxane derivative (V) in the presence of DCC and DMAP then provided the target ester.
📌 参考资料/链接:
参考文献标题:Taxoid reversal agents for drug-resistance in cancer chemotherapy and pharmaceutical compsns.thereof
文献作者:Bernacki,R.J.; Ojima,I.(State University of New York,Albany)
参考来源:EP 0966456; US 5811452; WO 9830553