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filingDate 1976-01-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1980-07-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber IE-42409-B1
titleOfInvention Acetylene derivatives of amino acids
abstract 1467138 Alkynoic acid derivatives RICHARDSON-MERRELL Inc 26 Jan 1976 [18 March 1975] 02855/76 Heading C2C Racemic and optically active compounds of the general formula (R = H, C 2-5 alkylcarbonyl or alkoxycarbonyl, COCH(NH 2 )R 10 ; R 2 = OH, C 1-8 alkoxy, C 1-4 alkylamino, NHCHR 4 COOH; R 4,10 =H, C 1-4 alkyl, benzyl, p-hydroxybenzyl; A=(CHR 1 ) n , CH=CH; R 1 = H, C 1-4 alkyl, phenyl optionally substituted by halogen, C 1-4 alkyl, C 1-4 alkoxy; n=1-5), the lactams of the compounds in which A=(CH 2 ) 2,3 and R=H, and their salts are prepared by standard methods, e.g. reacting CH 3 ) 3 SiC#CCH 2 N=CHPh with a haloester or unsaturated ester in the presence of a base to introduce the R 2 COA group followed by removal of the protecting groups and, optionally, introduction of an R substituent, replacement of R 2 by a different group, dehydration to a lactam, resolution and/or salt formation. The preparation of 3-benzylideneiminoprop-1- yne is described. The above compounds are useful in the treatment of disorders of the central nervous system and as hypothermic agents, myorelaxants, cholinergic agents, antibacterial agents, anticonvulsants, analgesics, anorectics, tranquillizers and sedatives. They may be administered in the form of pharmaceutical preparations containing them in association with a carrier.
priorityDate 1975-03-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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