发明名称 SYNTHESIS OF ASCAMYCIN
摘要 <p>PURPOSE:To obtain the titled compound which is an antibiotic substance for plants, by protecting the NH2 group of a specific adenosine derivative which is a starting raw material, and reacting the resultant compound with tert- butyloxycarbonyl-L-alanylimidazole and removing the protecting group. CONSTITUTION:2-Chloro-9-( 2', 3'-O-isopropylidene-5'-O-sulfamoyl-beta-D-ribofuranosyl) adenosine which is a starting raw material expressed by formula I is first reacted with di-tert-butyl bicarbonate, preferably at -78-+100 deg.C reaction temperature for 1-20hr reaction time to give a compound expressed by formula II (BOC is tert-butyloxycarbonyl), which is then subjected to coupling reaction with tert-butyloxycarbonyl-L-alanylimidazole to form a compound expressed by formula III. The resultant compound expressed by formula III is then treated with an acid, preferably trifluoroacetic acid to remove the protecting group and afford the aimed compound expressed by formula IV. The treatment with the acid is preferably carried out at -78-+100 deg.C for 0.5-20hr.</p>
申请公布号 JPS6256500(A) 申请公布日期 1987.03.12
申请号 JP19850196468 申请日期 1985.09.05
申请人 RIKAGAKU KENKYUSHO 发明人 ISONO KIYOSHI;UBUKATA MAKOTO
分类号 C07H19/167;A61K31/70;A61K31/7042;A61K31/7052;A61K31/7076;A61P31/04 主分类号 C07H19/167
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