- Preparation method of anticoagulation drug intermediate 5-methoxy-2-nitrobenzoic acid
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The invention discloses a preparation method of an anticoagulation drug intermediate 5-methoxy-2-nitrobenzoic acid and belongs to the field of drug intermediate synthesis. Cheap 3-drug intermediate serves as a raw material, a nitratlon reaction is selectively carried out at proper temperature to synthesize 5-chloro-2-nitrobenzoic acid, methyl alcohol is used for carrying out a substitution reaction on chlorine under the effect of alkali, and the needed intermediate 5-methoxy-2-nitrobenzoic acid is obtained. The preparation method which has short steps, simple reactions and low cost and can achieve stable industrial production is provided for a key intermediate of an anticoagulation drug Betrixaban.
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Paragraph 0026
(2017/08/28)
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- Effect of aldehyde and methoxy substituents on nucleophilic aromatic substitution by [18F]fluoride
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For a series of benzaldehydes only with a leaving group or with both a leaving group and a single methoxy substituent 18F-fluorination via nucleophilic aromatic substitution (SNAr) was studied in DMF and Me2SO. In general, the radiochemical yields were clearly higher in DMF than in Me2SO. In the fluorodehalogenation reaction (leaving group: halogen = Br, Cl), extremely low radiochemical yields were observed in Me2SO (2SO (within 3 min reaction time, 90% of the precursor was consumed; radiochemical yield = 1.0 ± 0.5%); however, in DMF oxidation was always kept at a low level during the entire reaction (13C-NMR ppm values of the aromatic carbon atom bearing the leaving group.
- Shen, Bin,L?ffler, Dirk,Zeller, Klaus-Peter,übele, Michael,Reischl, Gerald,Machulla, Hans-Jürgen
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p. 1461 - 1468
(2008/09/18)
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- 3-(3-aryloxyphenyl)-1-(substituted methyl)-s-triazine-2,4,6-oxo or thiotrione herbicidal agents
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There is provided a 3-(3-aryloxyphenyl)-1-(substituted methyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I STR1 Further provided are a composition and a method comprising that compound for the control of undesirable plant s
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- The synthesis of a novel series of substituted 2-phenyl-4H-3,1- benzoxazin-4-ones
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Following initial studies on a substituted 2-[3-methylphenyl]-4H-3,1- benzoxazin-4-one showing some cytotoxic activity, the synthesis of a novel series of 2-phenyl substituted 4H-3,1-benzoxazin-4-ones is reported herein.
- Pavlidis,Perry
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p. 533 - 548
(2007/10/02)
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- 1,2,3-Benzotriazin-4-ones and related systems. Part II. Thermolytic decomposition of substituted 1,2,3-benzotriazin-4-ones and isatoic anhydrides
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Several nuclear-substituted 1,2,3-benzotriazin-4-ones have been thermolysed in an inert solvent. In each case the major identifiable product proved to be a 2-(o-aminophenyl)-3,1-benzoxazin-4-one. Nuclear-substituted isatoic anhydrides on thermolysis behaved similarly.
- Archer, John G.,Barker, Alan J.,Smalley, Robert K.
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p. 1169 - 1173
(2007/10/06)
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