新产品编号:853207
Chemical Name: [2aR,4S,4aS,6R,9S(2R,3S),11S,12S,12aR,12bS]-6,12b-Diacetoxy-9-(3-benzamido-2-hydroxy-3-phenylpropionyloxy)-12-benzoyloxy-4-[2-[N,N-bis[2-[4-[4-[N,N-bis(2-chloroethyl)amino]phenyl]butyryloxy]ethyl]amino]acetoxymethoxy]-11-hydroxy-4a,8,13,13-tetramethyl-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-5-one
CAS No. 340722-62-5
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:The reaction of 2'-O-(triethylsilyl)paclitaxel (I) with dimethyl sulfide (DMS) and Bz2O2 in acetonitrile gives the 7-O-(methylsulfanylmethyl) derivative (II),which is condensed with chloroacetic acid (III) by means of N-iodosuccinimide (NIS) and Ag-OTf in THF to yield the 7-O-(chloroacetoxymethyl) derivative (IV).The desilylation of (IV) by means of HCl in acetonitrile affords the intermediate (V),which is finally condensed with the secondary amine (VI) by means of NaI in acetone to provide the target hybrid molecule.
📌 参考资料/链接:
参考文献标题:Synthesis and antitumor activity of novel paclitaxel-chlorambucil hybrids
文献作者:Wittman,M.D.; Kadow,J.F.; Vyas,D.M.; Lee,F.L.; Rose,W.C.; Long,B.H.; Fairchild,C.; Johnston,K.
参考来源:Bioorg Med Chem Lett 2001,11(6),811