地红霉素的合成
金洁，刘浚
(中国医学科学院 中国协和医科大学医药生物技术研究所 北京 100050)
[摘要]以红霉素A为原料，经红霉素腙路线合成红霉素胺，与2-(2-甲氧基乙氧基)乙缩醛一步缩合得到地红霉素，总收率为38.2%本研究对红霉素腙的合成方法及缩合反应的反应条件进行了改进。
[关键词] 地红霉素；大环内酯；合成
[中图分类号]R978.15 [文献标识码] B [文章编号]1003-3734(2001)-200630
Synthesis of dirithromycin
JIN Jie, LIU Jun
(Institute of Medicinal Biotechnology, Chinese Academy of Medicinal Sciences, Peking
Union Medical College, Beijing 100050 China)
[Abstract] Dirithromycin was synthesized from 9(s)-Erythromycylamine and 2-(2-methoxyethoxy)acetaldehy diethyl acetal by condensation with a total yield of 38.2%. 9(s)- Erythromycylamine was prepared from 9(s)-erythromycin hydroazone. The conditions of the erythromycin hydroazone and condensation were improved.
[Key Words] erythromycin; macrolide; synthesis
[作者简介]金洁(1962-)，女，主管技师，主要从事微生物药物的研制工作。联系电话：(010)63165267，E-mail：Ling.J@FM365.com。
[参考文献]
[1] Wildsmith, E.The reaction of erythromycin hydrazone with nitrous acid.A new route to erythromycylamine[J].Tetrahedron lett,1972,(1):29-30.
[2] Massay EH,Kitchell B,Martin LD,et al. Tetrahedron lett,1970,(2):157-160.
[3] Sigal M, Wiley P, Gerzon K, et al. Erythromycin degradation studies[J]. J Am Chem Soc, 1956,78: 388-395.
[4] Wildsmith E. Production of Erythromycylmine compounds[P]. US patent 3790599, 1974-02-05.
[5] Beal KF, Thor CJB. Water-soluble alkoxyacetals of polyvinyl Alcohl[J]. J Polymer Sci,1946,1(6): 540-548.
[6] McGill JM. One step process of dirthromycin[P]. EP 0535900A1, 1992-09-28
[7] Counter FT, Ensminger PD, Preston DA, et al. Synthesis and antimicrobial evaluation of dirthromycin, a new macrolide antibiotic derived from erythromycin[J]. Antimicrob Agents Chemother, 1991,35(6): 1116-1126., 百拇医药
(中国医学科学院 中国协和医科大学医药生物技术研究所 北京 100050)
[摘要]以红霉素A为原料，经红霉素腙路线合成红霉素胺，与2-(2-甲氧基乙氧基)乙缩醛一步缩合得到地红霉素，总收率为38.2%本研究对红霉素腙的合成方法及缩合反应的反应条件进行了改进。
[关键词] 地红霉素；大环内酯；合成
[中图分类号]R978.15 [文献标识码] B [文章编号]1003-3734(2001)-200630
Synthesis of dirithromycin
JIN Jie, LIU Jun
(Institute of Medicinal Biotechnology, Chinese Academy of Medicinal Sciences, Peking
Union Medical College, Beijing 100050 China)
[Abstract] Dirithromycin was synthesized from 9(s)-Erythromycylamine and 2-(2-methoxyethoxy)acetaldehy diethyl acetal by condensation with a total yield of 38.2%. 9(s)- Erythromycylamine was prepared from 9(s)-erythromycin hydroazone. The conditions of the erythromycin hydroazone and condensation were improved.
[Key Words] erythromycin; macrolide; synthesis
[作者简介]金洁(1962-)，女，主管技师，主要从事微生物药物的研制工作。联系电话：(010)63165267，E-mail：Ling.J@FM365.com。
[参考文献]
[1] Wildsmith, E.The reaction of erythromycin hydrazone with nitrous acid.A new route to erythromycylamine[J].Tetrahedron lett,1972,(1):29-30.
[2] Massay EH,Kitchell B,Martin LD,et al. Tetrahedron lett,1970,(2):157-160.
[3] Sigal M, Wiley P, Gerzon K, et al. Erythromycin degradation studies[J]. J Am Chem Soc, 1956,78: 388-395.
[4] Wildsmith E. Production of Erythromycylmine compounds[P]. US patent 3790599, 1974-02-05.
[5] Beal KF, Thor CJB. Water-soluble alkoxyacetals of polyvinyl Alcohl[J]. J Polymer Sci,1946,1(6): 540-548.
[6] McGill JM. One step process of dirthromycin[P]. EP 0535900A1, 1992-09-28
[7] Counter FT, Ensminger PD, Preston DA, et al. Synthesis and antimicrobial evaluation of dirthromycin, a new macrolide antibiotic derived from erythromycin[J]. Antimicrob Agents Chemother, 1991,35(6): 1116-1126., 百拇医药