http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1206088-A

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filingDate 1969-05-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1970-09-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1206088-A
titleOfInvention New pyrazolodiazepinone compounds and methods for their production
abstract 1,206,088. Pyrazolodiazepine derivatives. PARKE, DAVIS & CO. 29 May, 1969 [31 May, 1968], No. 27232/69. Heading C2C. Compounds of the general formula (R 1 =Me, Et; R 2 =alkyl(<4C), allyl; R 3 =H, Me; X 1 =H, Cl, CF 3 ) and their salts are prepared by (a) reacting a compound of the formula with a C 1-4 alkyl ester of glycine. or a salt thereof, (b) reacting a compound of the formula (X 2 =Br, Cl, I) or a salt thereof with ammonia, (c) cyclizing a compound (which may be prepared in situ) of the formula or (d) reacting a compound of the formula with X 2 CH 2 COX 3 (X 3 = Br, Cl) in the presence of a base, optionally followed in each case by methylation and/or salt formation with an acid or (when R 3 =H) base. The preparation of 1,3-dimethyl-4-nitropyrazole - 5 - carboxylic acid, 1 - ethyl - 3 - methyl- 4 - nitropyrazole - 5 - carboxylic acid, 1 - isopropyl - 3 - methyl - 4 - nitropyrazole - 5 - carboxylic acid, 3 - ethylpyrazole - 5 - carboxylic acid ethyl ester, 3-ethyl-1-methylpyrazole-5-carboxylic acid monohydrate, 3-ethyl-1-methyl-4-nitropyrazole - 5 - carboxylic acid, 1,3 - diethylpyrazole - 5 - carboxylic acid ethyl ester, 1,3- diethylpyrazole - 5 - carboxylic acid, 1,3 - diethyl - 4 - nitropyrazole - 5 - carboxylic acid, 4 - amino - -1 - ethyl - 3 - methylpyrazole - 5 - carboxylic acid, 5 - benzoyl - 1,3 - dimethyl - 4 - nitropyrazole, 5 - benzoyl - 1 - ethyl - 3 - methyl - 4 - nitropyrazole, 5 - benzoyl - 1 - isopropyl - 3 - methyl- 4 - nitropyrazole, 5 - benzoyl - 3 - ethyl - -1 - methyl- 4 - nitropyrazole, 5 - benzoyl - 1,3 - diethyl - 4 - nitropyrazole, 4 - amino - 5 - benzoyl - 1,3 - di - methylpyrazole and its hydrochloride, 4 - amino- 5 - benzoyl - 1 - ethyl - 3 - methylpyrazole and its hydrochloride monohydrate, 4 - amino - 5 - benzoyl - 1 - isopropyl - 3 - methylpyrazole and its hydrochloride, 4 - amino - 5 - benzoyl - 3 - ethyl- 1 - methylpyrazole, 4 - amino - 5 - benzoyl - 1,3- diethylpyrazole and its - hydrochloride, 4 - bromo - 1 - (2,3 - dibromopropyl) - 3 - methylpyrazole - 5 - carboxylic acid, 1 - allyl - 4 - bromo - 3 - methylpyrazole - 5 - carboxylic acid, 1 - allyl - 5 - benzoyl - 4 - bromo - 3 - methylpyrazole, 1 - allyl - 4 - amino - 5 - benzoyl - 3 - methylpyrazole, 4 - amino - 1 - ethyl - 3 - methyl- 5 - (α,α,α - trifluoro - o - toluoyl) pyrazole, 5- benzoyl - 4 - [2 - (carbobenzoxyamino) acetamido]- 1 - ethyl - 3 - methylpyrazole, 4 - (2 - aminoacetamido) - 5 - benzoyl - 1 - ethyl - 3 - methylpyrazole dihydrobromide, 5 - benzoyl - 4 - [2- (carbobenzoxyamino) acetamido] - 1,3 - dimethylpyrazole and 4 - (2 - aminoacetamido) - 5 - benzoyl - 1,3 - dimethylpyrazole is described. The compounds of the invention are central nervous system depressants, and may be administered in the form of pharmaceutical preparations containing them together with a carrier.
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priorityDate 1968-05-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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