- An Improved Rapid and Mild Deoxygenation of Amine N-oxides
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An improved mild and selective method for the deoxygenation of a variety of amine N-oxides has been carried out in the presence of silica gel under mild conditions at room temperature to afford corresponding amines in relatively good yields without purification. The reaction is tolerant of a variety of functional groups such as hydroxyl, ester, acid, carbonyl, and cyano groups, as well as halogens. This method would be of great utility to synthesize various pyridines and amines easily.
- Rajesh
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p. 486 - 491
(2017/12/29)
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- He holds the pyrrole department preparation method
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The invention belongs to the field of medicine and chemical engineering, and particularly relates to a preparation method for topiroxostat. 2-chloro-4-[(5-pyridine-4-yl)-1H-[1,2,4]triazole-3-yl]-pyridine is subjected to a cyanation reaction under the action of a cyanation reagent in the presence of a catalyst, base and a ligand to obtain topiroxostat. The preparation method comprises the following steps: 4-cyanopyridine-N-oxide is taken as a starting material, 1,2-dichloroethane is taken as a solvent, triethylamine is taken as base, phosphorus oxychloride is used as a chlorinated reagent, and chlorination is conducted to obtain 2-chloro-4-cyanopyridine; 2-chloro-4-cyanopyridine and isoniazide are in a methanol solvent, sodium methoxide is taken as a catalyst, and close-loop condensation is performed to obtain 2-chloro-4-[(5-pyridine-4-yl)-1H-[1,2,4]triazole-3-yl]-pyridine. The preparation method has the advantages that a safe and cheap cyanogroup source is selected, a hypertoxic cyanation reagent is avoided, the environmental harm is reduced, the product yield is high, the purity is high, and the suitability for industrial mass production is high.
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Paragraph 0031; 0035; 0036
(2018/04/01)
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- SUBSTITUTED ANTHRANILIC AMIDE DERIVATIVES AND METHODS OF USE
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Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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- Substituted alkylamine derivatives and methods of use
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Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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- Synthesis of substituted imidazoles
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The present invention prepares imidazoles by the selective closure of a keto-amide to form the imidazolyl ring. In particular, the present invention selectively closes a keto-amide substituted with three rings to form a tri-substituted imidazole.
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- Practical routes toward the synthesis of 2-halo- and 2-alkylamino-4-pyridinecarboxaldehydes
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We recently required an efficient synthesis of 2-halo- and 2-alkylamino-4-pyridinecarboxaldehydes. Several routes to these compounds were investigated resulting in efficient and practical procedures from readily available and inexpensive starting materials.
- Frey, Lisa F,Marcantonio, Karen,Frantz, Doug E,Murry, Jerry A,Tillyer, Richard D,Grabowski, Edward J.J,Reider, Paul J
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p. 6815 - 6818
(2007/10/03)
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- 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof
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Novel 6-heterocyclyl-pyrazolo[3,4-d]pyrimidin-4-ones, useful in treating cardiovascular disease, are prepared by reacting a 5-amino-1H-pyrazole-4-carboxamide with heterocyclylcarboxaldehyde or by reacting a 5-amino-1H-pyrazole-4-carbonitrile with a heterocyclylcarboxamidine, followed by diazotization and hydrolysis of the resulting 4-amino-6-heterocyclyl-pyrazolo[3,4-d]pyrimidine.
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