- A pyrazolopyridine compound and method for preparing the same
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The invention relates to a pyrazolopyridine compound and a preparation method thereof. The compound is 3-bromo-1H-pyrazolo[3,4-c]pyridine-7(6H)-one, and the preparation method comprises the following steps: (1) by taking the compound 1 2-chloro-3-amino-4methylpyridine as a starting raw material, etherifying 2-chloro-3-amino-4methylpyridine through sodium methoxide under the catalysis of copper iodide; (2) closing pyrazole ring through isoamyl nitrite; (3) feeding pyrazol-3 through NBS (N-Bromosuccinimide); (4) removing methoxyl to obtain phenyl (mixture difficult to separate) through pyridine hydrochloride; (5) performing acetyl protection to the obtained mixture so as to separate and purify; and (6) deacetylating through using potassium carbonate as a base to obtain a final product; and according to the preparation method, the mixture difficult to purify in the reaction process is conveniently separated and purified by adopting a method of performing protection and then removing protection, and the purification difficulty caused by instability of an intermediate product can be solved.
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Paragraph 0019; 0026
(2016/11/14)
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- A pyrazole compound pyridine and its preparation method
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The invention relates to a pyrazolo pyridine compound and a preparation method thereof. The pyrazolo pyridine compound is 3-bromine-7-hydroxy-pyrazolo pyridine. The preparation method comprises the following steps: (1) carrying out substitution reaction on 12-chlorine-4-methyl-3-aminopyridine as an initial raw material to form a compound 2; (2) carrying out ring closure on the compound 2 to form a compound 3, namely pyrazolo pyridine; (3) bromizing the compound 3 by adopting N-bromosuccinimide to obtain a compound 4; (4) forming the methoxyl of the compound 4 into a phenolic hydroxyl group by utilizing hydrochloric pyridine to obtain a compound 5a; (5) carrying out acetyl protection on the compound 5a to obtain a compound 6a; and (6) eliminating the acetyl protection on the compound 6 to obtain a final product, namely a compound 7. The obtained final product has a wide application prospect on the aspects of preventing and curing cancer.
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Paragraph 0025; 0026; 0033
(2018/01/19)
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- NEW POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTOR
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The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine alpha7 receptor.
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Page/Page column 12
(2013/02/28)
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- PYRAZOLOPYRIDINES USEFUL IN THE TREATMENT OF DISORDERS OF THE CENTRAL NERVOUS SYSTEM
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The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said com- pounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.
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Page/Page column 29
(2013/03/26)
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- Synthesis and antiviral activity evaluation of some novel acyclic C-nucleosides
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The preparation of novel 5-amino or 7-hydroxy substituted pyrazolo[4,3-b]pyridine and pyrazolo[3,4-c]pyridine acyclic C-nucleosides is described. Their synthesis was carried out by condensation of suitably substituted lithiated picolines with 2-benzyloxyethoxymethylchloride followed by pyrazole ring annulation. The compounds were evaluated for their antiviral activity against a wide panel of viruses, but were found inactive at subtoxic concentrations.
- Lougiakis, Nikolaos,Marakos, Panagiotis,Poul, Nicole,Balzarini, Jan
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scheme or table
p. 775 - 780
(2009/06/25)
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- Method for preparing alkyl-5,11-dihydro-6h-dipyrido[3,2-B:2',3'-E] [1,4] diazepin-6-ones
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A method for preparing certain 4-alkyl-5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-ones, which employs the following reaction scheme: STR1
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- Intermediates for making N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT)
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Compounds of the formula STR1 wherein R21 and R22 are as defined in the specification which are intermediates useful in the preparation of compounds of the formula STR2 and the pharmaceutically acceptable salts thereof, wherein Q and R1 are as defined in the specification. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
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- New N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase
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Compounds of the formula the pharmaceutically acceptable salts thereof, wherein Q and R1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
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