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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D317-72
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D495-10
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D317-72
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D495-10
filingDate 1968-12-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_81a14890386775a92d506460ca066d8d
publicationDate 1970-10-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1209799-A
titleOfInvention Aminoalkylbicyclocarboxylic acids
abstract 1,209,799. Aminomethylbicyclocarboxylic acids. MERCK & CO. Inc. 9 Dec., 1968 [14 Dec., 1967], No. 58306/68. Heading C2C. Novel compounds of formula wherein n is 2 or 3, X is H 2 or O, R<SP>1</SP> is H or alkanoyl and R‹ is H, a non-toxic esterifying group or a cation, and acid addition salts thereof, are prepared as in steps 9 and 11 of the reaction schemes below, optionally followed by acylation, esterification and/or salt formation where appropriate. Intermediates are prepared as in steps 1 to 8 and 10 of the reaction schemes below, wherein R is ethyl. The numbered reaction steps are as follows:- (1) Claisen condensation with NaOC 2 H 5 , (2) Reaction with NaH or other strong base followed by Br(CH 2 ) n Br, (3) Reaction with HS(CH 2 ) 2 SH in presence of BF 3 etherate in glacial acetic acid, (4) Reduction with Raney nickel, (5) Gentle saponification with a base such as NaOH in aqueous alcohol, (6) Reaction with triethylamine and chloroformic ester, followed by ammonia to convert the anhydride to the amide, (7) Dehydration with POCl 3 in 1,2-dichloroethane or pyridine, (8) Heat with base such as NaOH in aqueous alcohol, (9) Catalytic reduction, such as over Pt in aqueous alcoholic HCl solution, (10) Reaction with 1,2-ethylene glycol in presence of toluene sulfonic acid in benzene and (11) Heating with acid. Pharmaceutical compositions having antifibrinolytic activity being in conventional forms for oral and parenteral administration comprise an above novel compound and a carrier therefor. A method for treating disorders resulting from a pathological fibrolytic state using the novel compounds is also claimed for non-humans.
isCitedBy http://rdf.ncbi.nlm.nih.gov/pubchem/patent/FR-2085743-A1
priorityDate 1967-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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