- Synthetic method for 7-azaindole-3-methyl formate
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The invention discloses a synthetic method for 7-azaindole-3-methyl formate, and belongs to the field of organic synthesis. The method comprises the steps of reacting 2-amino-3-bromopyridine as a reactant with 3-hydroxyl acrylonitrile metal salt in an acidic environment to synthesize 3-(3-bromopyridine-2-yl-amino) acrylonitrile; adding 3-(3-bromopyridine-2-yl-amino) acrylonitrile, alkali and a catalysis system to a solvent, and performing a reaction to generate 3-cyano-7-azaindole; and finally performing a reaction in the presence of methanol and hydrochloric acid to obtain 7-azaindole-3-methyl formate. According to the method, the raw materials are low in price and easy to obtain, the reaction steps are simple, the reaction conditions are mild, the product quality is stable, and the purity is high; and therefore, the method is suitable for industrial production.
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- Synthesis process of 1H-pyrrolo[2,3-B] pyridine-3-carboxylic methyl ether
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The invention relates to a synthesis process of 1H-pyrrolo[2,3-B] pyridine-3-carboxylic methyl ether. The 1H-pyrrolo[2,3-B] pyridine-3-carboxylic methyl ether is obtained by the following steps: adding 1H-pyrrolo[2,3-B] pyridine-3-carboxylic acid and methanol to a three-mouth flask; firstly heating the three-mouth flask at 35-58 DEG C for 10-25 minutes, and adding a mixture prepared from anhydrous calcium chloride and nano-aluminum oxide as a catalyst; carrying out heating reflux at 45-62 DEG C for 25-60 minutes, carrying out esterification reaction, cooling to a room temperature, filtering and evaporating excessive methanol from the filtrate at a temperature not higher than 65 DEG C at reduced pressure, so as to obtain the 1H-pyrrolo[2,3-B] pyridine-3-carboxylic methyl ether. The adopted catalyst is convenient to operate when used, and is free of corrosivity or strong irritating smell, low in demands on hardware such as equipment, and beneficial to physical health of environmental personnel and operating personnel; the treatment after reaction is simple; the catalyst is low in price, available, low in cost and beneficial to large-scale application in industry.
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Paragraph 0017; 0018
(2017/01/09)
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- [4[4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL)-METHANONES AND SYNTHESIS THEREOF
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The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase including but not limited to for example asthma and other inflammatory diseases including age-related macular degeneration.
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Page/Page column 80; 81
(2011/07/09)
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- Desulfonylation of indoles and 7-azaindoles using sodium tert-butoxide
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A mild method for the desulfonylation of N-indoles and N-azaindoles is described. Deprotection is carried out under basic conditions, using sodium tert-butoxide in dioxane. Several functionalized indoles and 7-azaindoles were efficiently deprotected by this method, which is mild enough to be used to deprotect compounds including functions that are known to be sensitive to acidic or basic conditions.
- Chaulet, Charlotte,Croix, Cécile,Basset, Joan,Pujol, Maria-Dolores,Viaud-Massuard, Marie-Claude
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experimental part
p. 1481 - 1484
(2010/08/22)
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- PYRIDINONYL PDK1 INHIBITORS
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The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
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- COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
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The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
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Page/Page column 131-132
(2010/02/11)
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- 3-(GUANIDINOCARBONYL)HETEROCYCLE DERIVATIVES, PREPARATION PROCESS AND INTERMEDIATES OF THIS PROCESS, THEIR USE AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS INCLUDING THEM
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The present invention relates to the novel compounds of the formula (I) and their pharmaceutically acceptable salts. The inventive compounds are suitable, for example, as antiarrhythmic medicaments with a cardioprotective component for infarction prophyla
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