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固相合成甲胺基阿维菌素苯甲酸盐
引用本文:傅铭堃,吴宪,宁君,李建中.固相合成甲胺基阿维菌素苯甲酸盐[J].中国化学,2005,23(7):901-904.
作者姓名:傅铭堃  吴宪  宁君  李建中
作者单位:ResearchCenterforEco-environmentalSciences,ChineseAcademyofSciences,Beijing100085,China
摘    要:To implement the solid phase synthesis of 4““-epi-methylamino-4““-deoxyavermecfin B1 benzoate, tert-butyldimethylsilylchloride was chosen for the first solution synthesis. Then a novel silyl chloride resin 1, achieved from hydroxymethyl polystyrene resin and dimethyldichlorosilane, was used successfully for the attachment of avermectin B1 2. Through oxidation, amination formation, cleavage, and benzoate formation, resin bounded avermectin B1 9 gave 4““-epi-methylamino-4““-deoxyavermectin B1 benzoate 3.

关 键 词:固相合成  4“-表-甲氨基-4”-去氧avermectin  B1苯甲酸酯  支链丁基二甲基甲硅烷基氯化物  甲硅烷基醚
收稿时间:2004-8-31
修稿时间:2005-3-11

Solid Phase Synthesis of 4″‐epi‐Methylamino‐4″‐deoxyavermectin B1 Benzoate
Fu Ming‐Kun,Wu Xian,Ning Jun,Li Jian‐Zhong.Solid Phase Synthesis of 4″‐epi‐Methylamino‐4″‐deoxyavermectin B1 Benzoate[J].Chinese Journal of Chemistry,2005,23(7):901-904.
Authors:Fu Ming‐Kun  Wu Xian  Ning Jun  Li Jian‐Zhong
Abstract:To implement the solid phase synthesis of 4″‐epi‐methylamino‐4″‐deoxyavermectin B1 benzoate, tert‐butyl‐ dimethylsilylchloride was chosen for the first solution synthesis. Then a novel silyl chloride resin 1 , achieved from hydroxymethyl polystyrene resin and dimethyldichlorosilane, was used successfully for the attachment of avermectin B1 2 . Through oxidation, amination formation, cleavage, and benzoate formation, resin bounded avermectin B1 9 gave 4″‐epi‐methylamino‐4″‐deoxyavermectin B1 benzoate 6 .
Keywords:4″‐epi‐methylamino‐4″‐deoxyavermectin B1 benzoate  solid phase synthesis  silyl ether linker
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