http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1268608-A

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filingDate 1970-05-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1972-03-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1268608-A
titleOfInvention 5-amino-4-aroyl-1,3-dialkylpyrazoles
abstract 1,268,608. 4-Acyl-5-aminopyrazoles. PARKE DAVIS & CO. 13 May, 1970 [14 May, 1969; 30 March, 1970], No. 23088/70. Heading C2C. Novel compounds of Formula I and acid addition salts thereof wherein R 1 and R 2 are C 1-4 alkyl, R 3 is H or CH 3 and Ar is phenyl optionally substituted by Cl, Br, F, CF 3 , CH 3 or CH 3 O, or 2-chloro-3-methoxyphenyl, cyclohexyl or 2-thienyl, are prepared by one of the following methods (a) hydrolysis of an amide of Formula XIV (b) reaction of an amine R 3 NH 2 with a compound of Formula II wherein X is halogen, or (c) reaction of a compound of Formula XVI with a compound ArM where M is -Li or - Mg Halogen. Intermediates of Formula XIV above are prepared by reaction of a 4-unsubstituted-5- aminopyrazole with an acid chloride of formula ArCOCl and AlCl 3 . Intermediates of Formula II above are prepared either by reaction of an acid chloride and AlCl 3 with a compound of Formula VII or reaction of the compound of Formula VII with bromine in acetic acid to give the corresponding 4-bromo-compound-which is reacted with lithium butyl and the product then the acid chloride ArCOCl. Intermediates of Formula VII are prepared by action of a phosphorus oxyhalide on the 1,3- dialkyl-5-pyrazolone obtained by condensation of a hydrazine R 1 NHNH 2 and a compound Pharmaceutical compositions having a depressant effect on the central nervous system and an anticonvulsant activity in conventional forms for oral and parenteral administration comprise an above novel compound and a solid or liquid carrier or diluent.
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priorityDate 1969-05-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 36.