http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-325278-A1

Outgoing Links

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_03580d01b00ffd06ad2c36a210fa7575
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D333-38
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-38
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D333-38
filingDate 1966-04-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1967-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-325278-A1
titleOfInvention PROCEDURE FOR THE PREPARATION OF AMINOTIOPHENE DERIVATIVES
abstract Process for the preparation of amino-thiophene derivatives of the formula I ** (See formula) ** or its salts, where R means a phenyl residue containing one or more substituents, as substituents, halogen, trifluoromethyl, alkyl or alkoxy of low molecular weight, phenylalkoxy of low molecular weight in the alkyl part and optionally substituted in the phenyl nucleus by halogen, alkyl lower or lower alkoxy, or cycloalkyl with 5 to 6 carbon atoms, and two neighboring substituents being able to be members of a condensed alicyclic ring system, R1 is a carboxyl group, a carbonamide group or a carboxylic acid ester group, which in the ester group a) contains a low molecular weight alkyl residue, a low molecular weight dialkyl aminoalkyl residue or a low molecular weight alkyl amino alcohol residue with 4 to 5 carbon atoms in the ring, which may be interrupted by oxygen or by the > group N-CH3, or b) a phenyl radical optionally substituted by halogen, alkyl or low molecular weight alkoxy, or c) a phenylalkohyl residue of low molecular weight, and R2 and R3 represent hydrogen or low molecular weight alkyl, characterized in that a) a thiophanone of formula II ** (See formula) ** where R2 and R3 have the above-indicated significance and R4, in addition to the significances indicated for R1, can also be a cyan group, is condensed with a compound of the formula R-NH2 to form the corresponding 3-amino-2 derivative, 5-dihydro-thiophene, the product is dehydrogenated in known manner and, a cyan group optionally present in the radical R4, also in known manner, is transformed into a residue of the indicated significance for R1, or b) a thiophene derivative of formula III ** (See formula) ** which may also be partially or completely hydrogenated, is condensed with a compound of the formula IV R-Y IV where R2, R3 and R4 have the above-mentioned significance and, in each case, one of the radicals X and Y represents an amino group and the other a halogen atom, the product is optionally dehydrogenated and/or a cyan group optionally present in the rest R4 is transformed into the rest R1, or c) a compound of the formula V ** (See formula) ** which may also be totally or partially hydrogenated, in which R, R2, R3 and R4 have the above-mentioned significance and R5 represents an organic acid residue, is deacetylated, the product is optionally dehydrogenated and/or a cyano group optionally present in the rest R4, is transformed into the rest R1, the carboxyl functions R1 optionally present in the final products are transformed into other functions characterized by and/or, optionally, the free compounds are transformed with acids or bases into salts or the salts are transformed into the free compounds. (Machine-translation by Google Translate, not legally binding)
priorityDate 1965-04-10-04:00^^<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: 26.