Galamustine hydrochloride, G-6-M, C6-GalM, C6-GLM, C6-Galactose mustard
加莫司汀 Chemical Name: 6-[Bis(2-chloroethyl)amino]-6-deoxy-D-galactopyranose hydrochloride
CAS No. 107811-63-2, 105618-02-8 (free base)
项目整合开发状态: Phase I
项目研究机构: Georgetown University (Originator), Unimed (Originator), University of Pennsylvania (Originator)
合成路线:G-6-M is prepared as shown.All secondary hydroxyl groups of D-galactopyranose were protected by vicinal capping into bis(acetonides) yielding 1,2:3,4-di-O-isopropylidene-D-galactopyranose.This was tosylated at 6-CH2OH and alkylated at C-6 with diethanolamine.The hydroxyethyl groups of compound (II) were chlorinated and the acetonides deblocked with dilute aqueous acid to give 6-bis(2-chloroethyl)amino-6-deoxy-D-galactopyranose hydrochloride in an overall conversion of ca.42%.
📌 参考资料/链接:
参考文献标题:6-bis-(2-Chloroethyl)amino-6-deoxy-D-galactopyranose hydrochloride: Synthesis,chemical characterization,murine P388 antitumor activity,and bone marrow toxicity
文献作者:Schein,P.S.; Green,D.; Hammer,C.F.; McPherson,E.; Talebian,A.
参考来源:J Pharm Sci 1989,78(11),918-21
📄 详细内容
合成路线:G-6-M is prepared as shown.All secondary hydroxyl groups of D-galactopyranose were protected by vicinal capping into bis(acetonides) yielding 1,2:3,4-di-O-isopropylidene-D-galactopyranose.This was tosylated at 6-CH2OH and alkylated at C-6 with diethanolamine.The hydroxyethyl groups of compound (II) were chlorinated and the acetonides deblocked with dilute aqueous acid to give 6-bis(2-chloroethyl)amino-6-deoxy-D-galactopyranose hydrochloride in an overall conversion of ca.42%.
参考文献标题:Galamustine Hydrochloride
文献作者:Plasee,T.F.
参考来源:Drugs Fut 1991,16(3),205
产品链接: CAS No. 107811-63-2›› 产品链接: CAS No.105618-02-8››