JP2007070362A5 - - Google Patents

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JP2007070362A5
JP2007070362A5 JP2006298546A JP2006298546A JP2007070362A5 JP 2007070362 A5 JP2007070362 A5 JP 2007070362A5 JP 2006298546 A JP2006298546 A JP 2006298546A JP 2006298546 A JP2006298546 A JP 2006298546A JP 2007070362 A5 JP2007070362 A5 JP 2007070362A5
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Japan
Prior art keywords
nitrophenyl
fluoro
acid diester
malonic acid
difluoronitrobenzene
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Pending
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JP2006298546A
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Japanese (ja)
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JP2007070362A (en
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Priority to JP2006298546A priority Critical patent/JP2007070362A/en
Priority claimed from JP2006298546A external-priority patent/JP2007070362A/en
Publication of JP2007070362A publication Critical patent/JP2007070362A/en
Publication of JP2007070362A5 publication Critical patent/JP2007070362A5/ja
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Claims (8)

無機酸が炭酸である金属無機酸塩の存在下、一般式（１）
Figure 2007070362
（式中、Ｒ1、Ｒ2及びＲ3は、水素原子を示し、Ｘ1及びＸ2は、フッ素原子を示す。）
で示される２，４−ジフルオロニトロベンゼンに、一般式（２）
Figure 2007070362
（式中、Ｒ4は、アルコキシカルボニル基、アラルキルオキシカルボニル基又はアリールオキシカルボニル基を示し、Ｒ5は、アルキル基、アラルキル基又はアリール基を示す。）
で示されるマロン酸ジエステルを有機溶媒中で反応させることを特徴とする、一般式（３）
Figure 2007070362
（式中、Ｒ1、Ｒ2、Ｒ3、Ｒ4、Ｒ5及びＸ2は、前記と同義である。）
で示される２−（５−フルオロ−２−ニトロフェニル）マロン酸ジエステルの製造法。 In the presence of a metal inorganic acid salt in which the inorganic acid is carbonic acid, the general formula (1)
Figure 2007070362
(In the formula, R 1 , R 2 and R 3 represent a hydrogen atom, and X 1 and X 2 represent a fluorine atom.)
And 2,4-difluoronitrobenzene represented by the general formula (2)
Figure 2007070362
(Wherein, R 4 is an alkoxycarbonyl group, an aralkyloxycarbonyl group or an aryloxycarbonyl group, R 5 represents an alkyl group, an aralkyl group or an aryl group.)
Wherein the malonic acid diester represented by the general formula (3) is reacted in an organic solvent.
Figure 2007070362
(In the formula, R 1 , R 2 , R 3 , R 4 , R 5 and X 2 are as defined above.)
The manufacturing method of 2- (5-fluoro- 2-nitrophenyl) malonic acid diester shown by these. 無機酸が炭酸である金属無機酸塩の金属原子が、アルカリ金属原子である、請求項１に記載の２−（５−フルオロ−２−ニトロフェニル）マロン酸ジエステルの製造法。 The method for producing 2- (5-fluoro-2-nitrophenyl) malonic acid diester according to claim 1, wherein the metal atom of the metal inorganic acid salt whose inorganic acid is carbonic acid is an alkali metal atom. 無機酸が炭酸である金属無機酸塩が、炭酸ナトリウム又は炭酸カリウムである、請求項１又は２に記載の２−（５−フルオロ−２−ニトロフェニル）マロン酸ジエステルの製造法。 The method for producing 2- (5-fluoro-2-nitrophenyl) malonic acid diester according to claim 1 or 2, wherein the metal inorganic acid salt whose inorganic acid is carbonic acid is sodium carbonate or potassium carbonate. マロン酸ジエステルの使用量が、２，４−ジフルオロニトロベンゼンに対して１．０〜５．０倍モルである、請求項１〜３のいずれか１項に記載の２−（５−フルオロ−２−ニトロフェニル）マロン酸ジエステルの製造法。The 2- (5-fluoro-2) according to any one of claims 1 to 3, wherein the amount of malonic acid diester used is 1.0 to 5.0 times mol of 2,4-difluoronitrobenzene. -Nitrophenyl) Method for producing malonic acid diester. 無機酸が炭酸である金属無機酸塩の使用量が、２，４−ジフルオロニトロベンゼンに対して１．０〜５．０倍モルである、請求項１〜４のいずれか１項に記載の２−（５−フルオロ−２−ニトロフェニル）マロン酸ジエステルの製造法。The amount of the metal inorganic acid salt whose inorganic acid is carbonic acid is 1.0 to 5.0 times mol based on 2,4-difluoronitrobenzene, 2 according to any one of claims 1 to 4. A process for producing-(5-fluoro-2-nitrophenyl) malonic acid diester. 有機溶媒が、アセトニトリル、Ｎ，Ｎ−ジメチルホルムアミド及びジメチルスルホキシドからなる群より選択される１種以上である、請求項１〜５のいずれか１項に記載の２−（５−フルオロ−２−ニトロフェニル）マロン酸ジエステルの製造法。The organic solvent is one or more selected from the group consisting of acetonitrile, N, N-dimethylformamide, and dimethyl sulfoxide. Nitrophenyl) malonic acid diester production method. 有機溶媒の使用量が、２，４−ジフルオロニトロベンゼンに対して１〜５０重量倍である、請求項１〜６のいずれか１項に記載の２−（５−フルオロ−２−ニトロフェニル）マロン酸ジエステルの製造法。The 2- (5-fluoro-2-nitrophenyl) malon according to any one of claims 1 to 6, wherein the amount of the organic solvent used is 1 to 50 times by weight with respect to 2,4-difluoronitrobenzene. Method for producing acid diester. ２，４−ジフルオロニトロベンゼンにマロン酸ジエステルを２０〜１４０℃にて反応させる、請求項１〜７のいずれか１項に記載の２−（５−フルオロ−２−ニトロフェニル）マロン酸ジエステルの製造法。The production of 2- (5-fluoro-2-nitrophenyl) malonic acid diester according to any one of claims 1 to 7, wherein 2,4-difluoronitrobenzene is reacted with malonic acid diester at 20 to 140 ° C. Law.
JP2006298546A 2006-11-02 2006-11-02 Production method for 2-(5-chloro-2-nitrophenyl)-2-substituted acetate derivative Pending JP2007070362A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2006298546A JP2007070362A (en) 2006-11-02 2006-11-02 Production method for 2-(5-chloro-2-nitrophenyl)-2-substituted acetate derivative

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Application Number Priority Date Filing Date Title
JP2006298546A JP2007070362A (en) 2006-11-02 2006-11-02 Production method for 2-(5-chloro-2-nitrophenyl)-2-substituted acetate derivative

Related Parent Applications (1)

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JP2000239655A Division JP4000758B2 (en) 2000-07-19 2000-08-08 Process for producing 2- (5-halogeno-2-nitrophenyl) -2-substituted acetate derivative

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JP2007070362A JP2007070362A (en) 2007-03-22
JP2007070362A5 true JP2007070362A5 (en) 2007-08-23

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JP2006298546A Pending JP2007070362A (en) 2006-11-02 2006-11-02 Production method for 2-(5-chloro-2-nitrophenyl)-2-substituted acetate derivative

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* Cited by examiner, † Cited by third party
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EP0032620B2 (en) * 1979-12-19 1987-02-04 The Upjohn Company Process for preparing therapeutic 2-arylpropionic acids and esters, and novel arylmethylmalonate esters
JP4138067B2 (en) * 1998-02-17 2008-08-20 昭和化工株式会社 Method for producing methine derivative

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