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filingDate 1973-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1974-07-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1358680-A
titleOfInvention Pyrrolo-3,4-b-pyrazine derivatives
abstract 1358680 Pyrrolo-[3,4-b]pyrazine derivatives RHONE-POULENC SA 5 Jan 1973 [7 Jan 1972 9 Nov 1972] 796/73 Heading C2C Novel compounds of Formula I (in which A is a phenyl, pyridyl, pyridazinyl or 2-, 3- or 4-quinolyl radical, each radical optionally being substituted by one or more of halogen, C 1-4 alkyl, C 1-4 alkoxy, cyano and nitro, and n is 0 or 1) and acid addition salts thereof, are prepared (a) when n is 0, by reacting 1-chlorocarbonyl-4-methylpiperazine with an alkali metal salt of a compound of Formula II or (b) when n is 0, by reacting 1-methylpiperazine with a compound of Formula VI (in which Ar is phenyl optionally substituted by C 1-4 alkyl), and, if desired, converting a free base obtained by method (a), (b) or (c) into an acid addition salt. Compounds II are prepared by reacting pyrazine-2,3-dicarboxylic acid anhydride with an amine of formula H 2 N-A to produce a pyrazine-2,3-dicarboxylic acid derivative of Formula IV cyclizing this to produce an imide of Formula III and partially reducing this to give the desired compound II. Compounds VI are prepared by reacting a compound II with a chloroformate of formula Cl-CO-O-Ar. 2-Amino-7-chloroquinoline is prepared by reacting 2,7-dichloroquinoline with ammonia. Pharmaceutical compositions having tranquillizing and anticonvulsant activity, for oral, topical, rectal or parenteral administration comprise a compound of Formula I, or a pharmaceutically acceptable acid addition salt thereof, together with a pharmaceutical carrier or coating.
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priorityDate 1972-01-07-04:00^^<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: 42.