Atrimustine, Busramustine, Bestrabucil, KM-2210, Kregan
4H-1-苯并吡喃-6-乙酸,2-(4-氯苯基)-α-乙基-3-甲氧杂y-4-羰基-,甲基酯Chemical Name: (17beta)-Estra-1,3,5(10)-triene-3,17-diol 3-benzoate 17-[[4-[4-[bis(2-chloroethyl)amino]phenyl]-1-oxobutoxy]acetate]; 3-Benzoyloxy-17beta-[[4-[4-[bis(2-chloroethyl)amino]phenylbutyryloxy]acetoxy]-1,3,5(10)-estratriene
CAS No. 75219-46-4
项目整合开发状态: Phase III
项目研究机构: Kureha (Originator)
合成路线:The benzoylation of 1,3,5(10)-estratrien-3,17beta-diol (I) with benzoyl chloride (II) by means of NaOH in THF-water gives 3-benzoyloxy-1,3,5(10)-estratrien-17beta-ol (III),which is acylated with bromoacetyl bromide (IV) by means of pyridine in THF-CCl4 yielding 3-benzoyloxy-17beta-bromoacetoxy 1,3,5(10)-estratriene (V).Finally,this compound is condensed with silver 4-[4-[bis(2-chloroethyl)amino]phenyl]butyrate (VI) in DMSO.
📌 参考资料/链接：
参考文献标题:KM-2210
文献作者:Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1984,9(5),334
📄 详细内容
合成路线:The benzoylation of 1,3,5(10)-estratrien-3,17beta-diol (I) with benzoyl chloride (II) by means of NaOH in THF-water gives 3-benzoyloxy-1,3,5(10)-estratrien-17beta-ol (III),which is acylated with bromoacetyl bromide (IV) by means of pyridine in THF-CCl4 yielding 3-benzoyloxy-17beta-bromoacetoxy 1,3,5(10)-estratriene (V).Finally,this compound is condensed with silver 4-[4-[bis(2-chloroethyl)amino]phenyl]butyrate (VI) in DMSO.
参考文献标题:Novel estradiol compound,its preparation and anti-tumor agent containing the same
文献作者:Asano,K.; Tamura,H.; Tanaka,H.; Enomoto,S.
参考来源:BE 0878186; JP 55027121
产品链接: CAS No. 75219-46-4››