PNU-193821
Chemical Name: N-[5-[N-(2-Amidinoethyl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]-4-[4-[3-[4-(2-chloroethylsulfanyl)phenyl]-2(E)-propenamido]-1-methyl-1H-pyrrol-2-ylcarboxamido]-1-methyl-1H-pyrrole-2-carboxamide hydrochloride
CAS No. 257300-89-3 (free base)
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Reaction of 4-mercaptocinnamic acid (I) with 2-chloroethanol in the presence of NaOH afforded the hydroxyethyl sulfide (II),which was converted into the chloroethyl derivative (III) upon treatment with mesyl chloride and 37% HCl in hot pyridine.Coupling of carboxylic acid (III) with desformyldistamycin (IV) by means of DCC and HOBt gave rise to the title amide.
📌 参考资料/链接：
参考文献标题:Sulfurated distamycin derivs.,process for preparing them,and their use as antitumor agents
文献作者:Beria,I.; Caldarelli,M.; Capolongo,L.; Geroni,M.C.; Cozzi,P.(Pharmacia & Upjohn SpA)
参考来源:WO 0006541
📄 详细内容
合成路线:Reaction of 4-mercaptocinnamic acid (I) with 2-chloroethanol in the presence of NaOH afforded the hydroxyethyl sulfide (II),which was converted into the chloroethyl derivative (III) upon treatment with mesyl chloride and 37% HCl in hot pyridine.Coupling of carboxylic acid (III) with desformyldistamycin (IV) by means of DCC and HOBt gave rise to the title amide.
参考文献标题:Phenyl sulfur mustard derivatives of distamycin A
文献作者:Cozzi,P.; Beria,I.; Caldarelli,M.; Capolongo,L.; Geroni,C.; Mazzini,S.; Ragg,E.
参考来源:Bioorg Med Chem Lett 2000,10(15),1653