PA-457, YK-FH312

贝韦立马Chemical Name: [1S-(1alpha,3abeta,5aalpha,5bbeta,7aalpha,9beta,11abeta,11balpha,13abeta,13balpha)]-1-Isopropenyl-9-(3,3-dimethylsuccinyloxy)-5a,5b,8,8,11a-pentamethylperhydrocyclopenta[a]chrysene-3a-carboxylic acid; 3beta-(3-Carboxy-3-methylbutanoyloxy)lup-20(29)-en-28-oic acid
CAS No. 174022-42-5
项目整合开发状态: Phase I
项目研究机构: Biotech Research Laboratories (Originator), University of North Carolina (Originator), Panacos (Licensee), ViroLogic (Codevelopment)
合成路线:Betulinic acid (I) was extracted from the dried leaves of Syzygium claviforum.Acylation of (I) with 2,2-dimethylsuccinic anhydride (II) in the presence of DMAP in refluxing pyridine furnished the target 3?3?dimethylsuccinyl betulinic acid along with minor amounts of the undesired 2?2?dimethyl regioisomer (III),which were separated by means of preparative HPLC.
📌 参考资料/链接:
参考文献标题:Betulinic acid derivs.and uses thereof
文献作者:Lee,K.-H.; Kashiwada,Y.; Hashimoto,F.; Cosentino,L.M.; Manak,M.(Biotech Research Laboratories; University of North Carolina)
参考来源:US 5679828; WO 9639033

📄 详细内容


合成路线:Betulinic acid (I) was extracted from the dried leaves of Syzygium claviforum.Acylation of (I) with 2,2-dimethylsuccinic anhydride (II) in the presence of DMAP in refluxing pyridine furnished the target 3?3?dimethylsuccinyl betulinic acid along with minor amounts of the undesired 2?2?dimethyl regioisomer (III),which were separated by means of preparative HPLC.

参考文献标题:Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents
文献作者:Kashiwada,Y.; Hashimoto,F.; Cosentino,L.M.; Chen,C.H.; Garrett,P.E.; Lee,K.H.
参考来源:J Med Chem 1996,39(5),1016


合成路线:Betulinic acid (I) was extracted from the dried leaves of Syzygium claviforum.Acylation of (I) with 2,2-dimethylsuccinic anhydride (II) in the presence of DMAP in refluxing pyridine furnished the target 3?3?dimethylsuccinyl betulinic acid along with minor amounts of the undesired 2?2?dimethyl regioisomer (III),which were separated by means of preparative HPLC.

参考文献标题:Anti-AIDS agents.30.Anti-HIV activity of oleanolic acid,pomolic acid,and structurally related triterpenoids
文献作者:Kashiwada,Y.; Wang,H.K.; Nagao,T.; Kitanaka,S.; Yasuda,I.; Fujioka,T.; Yamagishi,T.; Cosentino,L.M.; Kozuka,M.; Okabe,H.; Ikeshiro,Y.; Hu,C.Q.; Yeh,E.; Lee,K.H.
参考来源:J Nat Prod 1998,61(9),1090


合成路线:Betulinic acid (I) was extracted from the dried leaves of Syzygium claviforum.Acylation of (I) with 2,2-dimethylsuccinic anhydride (II) in the presence of DMAP in refluxing pyridine furnished the target 3?3?dimethylsuccinyl betulinic acid along with minor amounts of the undesired 2?2?dimethyl regioisomer (III),which were separated by means of preparative HPLC.
参考文献标题:Anti-AIDS agents - XXVII.Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives
文献作者:Hashimoto,F.; Kashiwada,Y.; Cosentino,L.M.; Chen,C.H.; Garrett,P.E.; Lee,K.H.
参考来源:Bioorg Med Chem 1997,5(12),2133


产品链接: CAS No. 174022-42-5››