Methylprednisolone aceponate, SH-440, ZK-91588, Adventan, Advantan
甲基泼尼松龙乙丙酸酯Chemical Name: (6alpha,11beta)-21-Acetoxy-11-hydroxy-6-methyl-17-(propionyloxy)pregna-1,4-diene-3,20-dione
CAS No. 86401-95-8
项目整合开发状态: Launched-1992
项目研究机构: Leiras (Originator), Schering AG (Originator)
合成路线:The esterification of 11beta,17alpha,21-trihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione (I) with triethyl orthopropionate (II) by means of pyridinium tosylate in DMF - benzene gives the corresponding cyclic diester (III),which is partially hydrolyzed with acetic acid - sodium acetate in methanol - water,yielding the 17alpha-propionyloxy derivative (IV).Finally,this compound is acetylated with acetic anhydride and pyridine.
📌 参考资料/链接：
参考文献标题:New 6alpha-methylprednisolone derivs.their preparation and use
文献作者:Annen,K.; Petzoldt,K.; Laurent,H.; Wiechert,R.; Hofmeister,H.; Wendt,H.(Schering AG)
参考来源:EP 0072547
📄 详细内容
合成路线:The esterification of 11beta,17alpha,21-trihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione (I) with triethyl orthopropionate (II) by means of pyridinium tosylate in DMF - benzene gives the corresponding cyclic diester (III),which is partially hydrolyzed with acetic acid - sodium acetate in methanol - water,yielding the 17alpha-propionyloxy derivative (IV).Finally,this compound is acetylated with acetic anhydride and pyridine.
参考文献标题:Methylprednisolone Aceponate
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1993,18(2),130
合成路线:The esterification of 11beta,17alpha,21-trihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione (I) with triethyl orthopropionate (II) by means of pyridinium tosylate in DMF - benzene gives the corresponding cyclic diester (III),which is partially hydrolyzed with acetic acid - sodium acetate in methanol - water,yielding the 17alpha-propionyloxy derivative (IV).Finally,this compound is acetylated with acetic anhydride and pyridine.
参考文献标题:Studies on topical antiinflammatory corticosteroids.I.Syntheses and vasoconstrictive activities of 11beta,17alpha,21-trihydroxy-6alpha-methyl-1,4-pregnadiene-3,20-dione 17-ester and 17,21-diester derivatives
文献作者:Sugai,S.; Okazaki,T.; Kajiwara,Y.; Kanbara,T.; Naito,Y.; Yoshida,S.; Akaboshi,S.; Ikegami,S.; Kamano,Y.
参考来源:Chem Pharm Bull 1985,33(5),1889
产品链接: CAS No. 86401-95-8››