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2. 发明专利

JPS60190787A Sialic acid derivative and its preparation 失效
标题翻译：酸性衍生物及其制备方法
公开(公告)号：JPS60190787A
公开(公告)日：1985-09-28
申请号：JP4490584
申请日：1984-03-09
申请人： Kanto Ishi Pharma Co Ltd , Rikagaku Kenkyusho
发明人： OGAWA TOMOYA , FUJIKURA KAZUSHIGE , SUGIMOTO MAMORU , SHIDORI YOSHIYASU , ITOU MASAYOSHI
IPC分类号： C07H15/10 , A61K31/70 , A61K31/7028 , A61P31/04 , C07H15/04 , C07H15/18
CPC分类号： Y02P20/55
摘要： NEW MATERIAL:A compound shown by the formula I (R
1 is H, or CH
3 ; R
2 is acyl, or n-propyl; R
3 and R
4 are H, D-glucopyranosyl, 2,3,4-tri-O-benzyl-D-glycopyranosyl, 2,3,4-tri-O-benzyl-6-O-monochloroacetyl-D-glucopyranosyl, benzoyl, or benzyl; R
5 and R
6 are linked to form isopropylidene, or benzylidene; Ac is acetyl).
USE: A remedy for meningitis.
PREPARATION: A compound shown by the formula II is deacetylated, reacted with 2,2-dimethoxypropane to give a novel compound shown by formula III, which is reacted with a compound shown by the formula IV (X is halogen, Br is benzyl; MCA is monochloroacetyl) in a solvent such as 1,2-dichloroethane, etc. in the presence of glycosidation catalyst such as Hg(CH)
2 , etc. at -20W150°C for 1W120hr, and if necessary, the protecting group is removed, or reduced, to give a compound shown by the formula I .
COPYRIGHT: (C)1985,JPO&Japio
摘要翻译：新材料：由式I表示的化合物（R1为H或CH3; R2为酰基或正丙基; R3和R4为H，D-吡喃葡萄糖基，2,3,4-三-O-苄基-D - 吡喃葡萄糖基，2,3,4-三-O-苄基-6-O-单氯乙酰基-D-吡喃葡萄糖基，苯甲酰基或苄基; R5和R6连接形成异亚丙基或亚苄基; Ac是乙酰基。使用：脑膜炎的补救措施。制备：式II化合物脱乙酰化，与2,2-二甲氧基丙烷反应，得到式III所示的新化合物，其与式IV化合物（X为卤素，Br为苄基; MCA 是一氯乙酰基）在溶剂如1,2-二氯乙烷等中，在糖化催化剂如Hg（CH）2等存在下，在-20-150℃下反应1-120小时，如果需要，除去或还原保护基，得到式I所示的化合物。

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