http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-351511-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_6b6fc801b5bfe5304ffa40d938db6e09 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-535 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D265-36 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-535 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D265-36 |
| filingDate | 1968-03-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1969-06-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-351511-A1 |
| titleOfInvention | PROCEDURE FOR THE PREPARATION OF MORPHOLIN DERIVATIVES. |
| abstract | Novel morpholine derivatives of the formula wherein X is H, OH or NH 2 and Am is NH 2 , C 1-4 alkylamine, di C 1-4 alkylamino, polymethyleneimino group having 5-8 ring members and optionally substituted by one or more alkyl groups having 1 to 4 carbon atoms, or morpholino and their addition salts with inorganic and organic acids are prepared by reacting the corresponding ester in which Am is replaced by -OR, where R is a C 1-6 alkyl group with ammonia or an amine of the formula AmH. The diastereoisomeric ethyl esters of d,l-cis (diequat.) - 6 - C3,4 - methylenedioxyphenyl)- 2- morpholine lactic acid are obtained by the hydrogenolysis of the corresponding isomers of d,l - cis (equat.) - 4 - benzyl - 6 - (3.4 - methylenedioxyphenyl) - 2 - morpholine lactic acid ethyl esters, separated from each other by thin layer chromatography,and prepared by the hydrolysis and esterification of d,l - cis (diequat.) - 4- benzyl - 6 - (3,4 - methylenedioxyphenyl) - 2- morpholine acetaldehyde cyanohydrin, which is in turn obtained by reacting KCN with the corresponding aldehyde derivative resulting from the hydrolysis of its diethyl acetal compound, said acetal being prepared by the cyclization of 4-[N- benzyl - N - (3,4 - methylenedioxy - # - hydroxyphenylethyl) - amino] - 3 - hydroxybutyraldehyde diethyl acetal, obtained by refluxing an ethanol solution of 1,1-diethoxy-3,4-epoxy-butane and 3,4 - methylenedioxy - [alpha] - (benzylaminomethyl) benzyl alcohol the latter compound resulting from the reduction with sodium borohydride of 3,4 - methylenedioxy - [alpha] - (benzylideneaminomethyl-benzyl alcohol formed by the elimination of water between [alpha]-aminomethyl-3,4-methylenedioxybenzyl alcohol and benzaldehyde. Pharmaceutical compositions, having hypotensive activity and suitable for oral, parenteral or rectal administration, contain the above novel morpholine compounds or acid addition salts thereof as the active ingredient. |
| priorityDate | 1967-03-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 30.