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1. 发明专利

JPS58192867A Preparation of omega-indol-3-yl-alkanol compound 失效
标题翻译： OMEGA-INDOL-3-YL-ALKANOL化合物的制备
公开(公告)号：JPS58192867A
公开(公告)日：1983-11-10
申请号：JP7450082
申请日：1982-05-06
申请人： Kawaken Fine Chem Co Ltd
发明人： TAKANASHI KOUJI , KUBO MASAAKI
IPC分类号： C07D209/12
摘要： PURPOSE: To prepare the titled compound, in high yield, by reacting a phenylhydrazine compound with a specific amount of an oxacycloalkan-2-ol compound in the presence of the necessary amount of a strong acid to convert the mixture to hydrochloride.
CONSTITUTION: The objective compound of formula VI is prepared by reacting (A) 1mol of a phenylhydrazine compound of formula I (R
1 is H, lower alkyl, aryl, or aralkyl; R
2 is R
1 , lower alkoxy, aryloxy, aralkoxy, or halogen) with (B) 1.1W 3mol of one or more oxacycloalkan-2-ol compounds of formula II [R
3 is H or lower alkyl; R
4 is group of formula III (R
7 is H or lower alkyl; k is 0W2) or formula IV; R
5 is lower alkyl; n is 0 or 1] or formula V (R
6 is H or CH
3 ; l is 1 or 2), in a solvent containing one or more alcoholic compounds in the presence of a specific amount of a strong acid at 70W170°C for 30minW several hours.
USE: Raw material indole derivatives, etc.
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：目的：为了以高产率制备标题化合物，通过使苯肼化合物与特定量的氧杂环烷-2-醇化合物在必要量的强酸存在下反应，将混合物转化成盐酸盐。结构式：式Ⅵ的目标化合物是通过使（A）1摩尔式I的苯肼化合物（R 1为H，低级烷基，芳基或芳烷基; R 2为R 1，低级烷氧基，芳氧基，芳烷氧基或卤素）与（B）1.1-3mol的一种或多种式Ⅱ的氧杂环烷-2-醇化合物[R3是H或低级烷基; R4是式III的基团（R7是H或低级烷基; k是0-2）或式IV; R5是低级烷基; 在特定量的强酸存在下，在70-170℃下，在含有一种或多种醇化合物的溶剂中，n为0或1]或式V（R 6为H或CH 3; l为1或2） 30分钟 - 数小时。用途：原料吲哚衍生物等

2. 发明专利

JPS5973568A Preparation of tryptamine compound 失效
标题翻译：木霉素化合物的制备
公开(公告)号：JPS5973568A
公开(公告)日：1984-04-25
申请号：JP18306682
申请日：1982-10-19
申请人： Kawaken Fine Chem Co Ltd
发明人： TAKANASHI KOUJI , KUBO MASAAKI
IPC分类号： C07D209/16
摘要： PURPOSE: To obtain advantageously the titled compound which is a synthetic raw material for indole derivatives and medicines, etc., by reacting an easily available cyclopropylcarbonyl compound as a starting raw material with a phenylhydrazine compound in a solvent under acidic conditions.
CONSTITUTION: A cyclopropylcarbonyl compound of formula I (R
1 is H, alkyl, aryl or aralkyl) is reacted with a phenylhydrazine compound of formula II(R
2 is H, alkyl, aryl or aralkyl; R
3 is H, alkyl, aryl, aralkyl, alkoxyl or aralkyloxy, etc.) in the presence of a solvent, e.g. ethanol or ethylene glycol monomethyl ether, under acidic conditions with sulfuric acid, p-toluenesulfonic acid, etc. at 70W200°C to give the aimed compound of formula III. The compound of formula I can be easily synthesized from cyclopropanecarbonitrile, etc.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：为了获得作为吲哚衍生物和药物等的合成原料的标题化合物，通过在酸性条件下，在溶剂中使易于得到的起始原料的环丙基羰基化合物与苯肼化合物反应。构型：将式I的环丙基羰基化合物（R 1是H，烷基，芳基或芳烷基）与式II的苯肼化合物反应（R2是H，烷基，芳基或芳烷基; R3是H，烷基，芳基，芳烷基，烷氧基或芳烷氧基等）在溶剂存在下进行乙醇或乙二醇单甲醚，在酸性条件下，用硫酸，对甲苯磺酸等在70-200℃下反应，得到目的化合物Ⅲ。式I的化合物可以从环丙腈等容易地合成

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