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1. 发明专利

JPS5748912A Antiulcer agent 失效
标题翻译：抗体药剂
公开(公告)号：JPS5748912A
公开(公告)日：1982-03-20
申请号：JP12497580
申请日：1980-09-08
申请人： Sumitomo Chem Co Ltd
发明人： SUGIE AKIHIKO , KAWAKAMI HAJIME , FUKUDA TOKUO , ONO KEIICHI , AONO SHIYUNJI , KATSUBE SUMIMOTO
IPC分类号： A61K31/19 , A61K31/215 , A61P1/04
摘要： NEW MATERIAL:A compound of formula I (R
1 is H or 1W4C lower alkyl) and a salt thereof.
EXAMPLE: The compound of formula II.
USE: A chemically stable antiulcer agent, having excellent selectivity, with little side effects, and useful for diseases, e.g. duodenal ulcer, and administrable orally and parenterally.
PROCESS: As shown in the reaction formulas, a cyclohexene derivative of formula III is subjected to the oxidative ring cleavage to give a dialdehyde derivative of formula IV, which is then subjected to the intramolecular aldol reaction to afford a compound of formula V. The resultant compound of formula V is then reacted with a wittig reagent to give a compound of formula VI, which is subsequently reduced to afford a compound of formula VII. The protecting group of the ketal ketonic group expressed by W is then removed from the resultant compound of formula VII to give a compound of formula VIII, which is then reacted with a Wittig reagent to afford the compound of formula I.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：式Ⅰ化合物（R1为H或1-4C低级烷基）及其盐。实施例：式II化合物。用途：化学稳定的抗溃疡剂，具有优异的选择性，副作用小，可用于疾病，例如十二指肠溃疡，口服和肠胃外给药。方法：如反应式所示，将式III的环己烯衍生物进行氧化环切割，得到式IV的二醛衍生物，然后将其进行分子内醛醇缩合反应，得到式V化合物。所得物然后将式V化合物与无机试剂反应，得到式Ⅵ化合物，随后将其还原，得到式Ⅶ化合物。然后将由W表示的缩酮酮基团的保护基从所得到的式VII化合物中除去，得到式VIII化合物，然后与Wittig试剂反应，得到式I化合物。

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