JPS5750962A - Novel preparation of isoindoline derivative - Google Patents
Novel preparation of isoindoline derivativeInfo
- Publication number
- JPS5750962A JPS5750962A JP12752980A JP12752980A JPS5750962A JP S5750962 A JPS5750962 A JP S5750962A JP 12752980 A JP12752980 A JP 12752980A JP 12752980 A JP12752980 A JP 12752980A JP S5750962 A JPS5750962 A JP S5750962A
- Authority
- JP
- Japan
- Prior art keywords
- derivative
- high yield
- formula
- reaction
- agent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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- Indole Compounds (AREA)
Abstract
PURPOSE: To prepare the titled compound having excellent activity as an antiphlogistic agent and analgesic agent, in high yield, by cyclizing the benzylidene derivative derived from an o-phthalaldehydic acid ester derivative and an aniline derivative in high yield, with a reducing agent.
CONSTITUTION: The o-phthalaldehydic acid ester of formula I (R1 is lower alkyl) is made to react with the aniline derivative of formula II (R2 is H or lower alkyl; X is carboxy, carboalkoxy, amido, or cyano) in a solvent such as methanol for a short time at room temperature of under slight heating to obtain the benzylidene derivative of formula III in high yield. The resultant derivative is, without isolating from the reaction mixture, reacted and cyclized at 20W40°C for 1W24hr in the presence of a reducing agent such as NaBH4 to obtain the objective compound of formula IV, such as 1-oxo-2-[p-[(α-methyl)carboxymethyl]-phenyl]-isoindoline, in high yield.
EFFECT: The reaction can be carried out at room temperature in one bath, and the apparatus and operation of the reaction are also simple and economical.
COPYRIGHT: (C)1982,JPO&Japio
Priority Applications (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP12752980A JPS5750962A (en) | 1980-09-10 | 1980-09-10 | Novel preparation of isoindoline derivative |
US06/299,432 US4400520A (en) | 1980-09-10 | 1981-09-04 | Novel process for preparing isoindoline derivatives |
EP81304119A EP0047674B1 (en) | 1980-09-10 | 1981-09-09 | Novel process for preparing isoindolin derivatives |
DE8181304119T DE3162438D1 (en) | 1980-09-10 | 1981-09-09 | Novel process for preparing isoindolin derivatives |
CA000385540A CA1155448A (en) | 1980-09-10 | 1981-09-09 | Process for preparing isoindolin derivatives |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP12752980A JPS5750962A (en) | 1980-09-10 | 1980-09-10 | Novel preparation of isoindoline derivative |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS5750962A true JPS5750962A (en) | 1982-03-25 |
Family
ID=14962266
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP12752980A Pending JPS5750962A (en) | 1980-09-10 | 1980-09-10 | Novel preparation of isoindoline derivative |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS5750962A (en) |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS55149256A (en) * | 1979-05-10 | 1980-11-20 | Hisamitsu Pharmaceut Co Inc | Novel preparation of isoindoline derivative |
-
1980
- 1980-09-10 JP JP12752980A patent/JPS5750962A/en active Pending
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS55149256A (en) * | 1979-05-10 | 1980-11-20 | Hisamitsu Pharmaceut Co Inc | Novel preparation of isoindoline derivative |
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