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1. 发明专利

JPH0380155B2 失效
公开(公告)号：JPH0380155B2
公开(公告)日：1991-12-24
申请号：JP18610584
申请日：1984-09-05
申请人： RIKAGAKU KENKYUSHO
发明人： OOISHI TAKESHI , NAKADA TADASHI , SAITO KUNIO , NAGAO SHIGETO , MORI NOBUYUKI
IPC分类号： C07D407/06 , C07D309/00 , C07D317/00

2. 发明专利

JPH0528713B2 失效
公开(公告)号：JPH0528713B2
公开(公告)日：1993-04-27
申请号：JP22557484
申请日：1984-10-26
申请人： RIKAGAKU KENKYUSHO
发明人： OOISHI TAKESHI , NAKADA TADASHI , NAGAO SHIGETO , MORI NOBUYUKI
IPC分类号： C07F7/18 , C07D309/08 , C07D309/10

3. 发明专利

JPS6163675A Novel lactone compound and its synthesis 失效
标题翻译：新型Lactone化合物及其合成
公开(公告)号：JPS6163675A
公开(公告)日：1986-04-01
申请号：JP18610584
申请日：1984-09-05
申请人： Rikagaku Kenkyusho
发明人： OISHI TAKESHI , NAKADA TADASHI , SAITO KUNIO , NAGAO SHIGETO , MORI NOBUYUKI
IPC分类号： C07D407/06 , C07D309/00 , C07D317/00
摘要： NEW MATERIAL:The lactone compound of formula I (Me is methyl).
USE: Useful for the synthesis of a fragment compound corresponding to the 3W10C part of ionophore antibiotic substance, boromycin and aplasmomycin which are natural physiologically active substances having antibacterial activity.
PREPARATION: The compound of formula I can be prepared by (1) oxidizing the compound of formula II to an aldehyde compound, (2) reacting the aldehyde with lithium diisopropylamide and the compound of formula III, (3) treating the obtained compound of formula IV with an acid to afford the compound of formula V, (4) reacting the product successively with tert-butyldiphenylsilyl chloride, vinyl ethyl ether, and orthoformic acid ester, (5) reacting the resultant compound of formula VI with propanedithiol in the presence of a Lewis acid, and then with 2,2-dimethoxypropane, (6) removing the dithiol group, (7) methylating the product, and finally (8) treating with an alcoholate.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：新材料：式I的内酯化合物（Me是甲基）。用途：用于合成对应于具有抗菌活性的天然生理活性物质的离子载体抗生素物质，硼霉素和阿曲霉素的3-10C部分的片段化合物。制备：式I化合物可以通过（1）将式II化合物氧化成醛化合物，（2）使醛与二异丙基氨基锂和式III化合物反应，（3）将所得式 IV与酸反应，得到式V化合物，（4）使产物依次与叔丁基二苯基甲硅烷基氯，乙烯基乙基醚和正己酸酯反应，（5）使所得到的式VI化合物与丙二硫醇在路易斯酸，然后用2,2-二甲氧基丙烷，（6）除去二硫醇基，（7）甲基化产物，最后（8）用醇化物处理。

4. 发明专利

JPS61103879A Synthesis of optically active (+)-pedamide 失效
标题翻译：光学活性（+） - PEDAMIDE的合成
公开(公告)号：JPS61103879A
公开(公告)日：1986-05-22
申请号：JP22557484
申请日：1984-10-26
申请人： Rikagaku Kenkyusho
发明人： OISHI TAKESHI , NAKADA TADASHI , NAGAO SHIGETO , MORI NOBUYUKI
IPC分类号： C07F7/18 , C07D309/08 , C07D309/10
摘要： PURPOSE: To obtain a pedamide which is a fragment compound of pederine having specific steric structure and physiological activity, in high stereoselectivity and yield, from a starting substance producible from optically active l-malic acid via novel intermediates in 15 steps.
CONSTITUTION: The optically active (+)-pedamide of formula VI can be prepared economically in high optical yield and reaction yield, by (1) converting the compound of formula I to the novel substance of formula IV via the compound of formula II (Me is methyl; Et is ethyl), the compound of formula III (ϕ is phenyl;
t Bu is t-butyl), its ethoxyethyl derivative, hemiacetal, 4β-alcohol, β-thioacetal-δ-lactone, dimethoxy derivative, lactol, methoxymethyl ether, dimethoxy ketone and dimethoxy alcohol all of which are novel substances, (2) converting the compound of formula IV to the novel substance of formula V (Ac is acetly) by demethoxymethylation followed by acetylation, (3) nitrilating the OAc group of the compound of formula V and finally (4) hydrolyzing the product.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：通过15个步骤，通过新型中间体，从可从光学活性的苹果酸生产的起始物质中获得具有特定立体选择性和产率的具有特定立体选择性和生理活性的er菜片段化合物的西酞酰胺。构成：式VI的光学活性（+） - 酰胺可以经济地制备，具有高的光学收率和反应产率，通过（1）通过式II化合物（I）将式I化合物转化成式IV的新物质是甲基; Et是乙基），式III化合物（phi是苯基; Bu是叔丁基），其乙氧基乙基衍生物，半缩醛，4beta醇，β-硫代缩醛-δ-内酯，二甲氧基衍生物，内酯，甲氧基甲基醚，二甲氧基酮和二甲氧基醇，都是新物质，（2）通过脱甲氧基甲基化，然后乙酰化将式IV化合物转化为式V的新物质（Ac为乙酰基），（3）将OAc基团腈化的式V化合物，最后（4）水解产物。

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