EP 0000035 A1 19781220 - Alpha-amino acids, compositions and process for preparing said compounds.
Title (en)
Alpha-amino acids, compositions and process for preparing said compounds.
Title (de)
Alpha-Aminosäuren, Präparate und Verfahren zur Herstellung dieser Verbindungen.
Title (fr)
Alpha-amino-acides, compositions et procédé pour la préparation de ces composés.
Publication
Application
Priority
US 80239077 A 19770601
Abstract (en)
alpha -Amino Acids, compositions and process for preparing said compounds alpha -ethynyl- and - alpha -vinyl-3,4-disubstituted pheynylalanines and esters thereof, have been prepared by reaction of methyl 3,4-dihydroxybenzoate with diphenyldichloromethane, reduction of the so obtained methyl 3,4-diphenylmethylene- dioxy- benzoate to 3,4-diphenylmethylenedioxybenzyl- alcohol, and transforming this to the benzylchloride. This 3,4-diphenylmethylenedioxybenzylchloride reacts with 1-trimethyl- silyl-N-benzylidene-3-aminoprop-1-yne to form 3-(3,4- diphenylmethylenedioxybenzyl) -1-trimethysilyl N-benzylidene-3- aminoprop-1-yne. <??>With methyl chloroformate this compound gives 3-carbomethoxy-3- (3, 4- diphenylmethylenedioxybenzyl-1-trimethylsilyl-N-benzylidene -3-aminoprop-1-yne. <??>The benzylidene-group, the trimethylsilyl-group and the diphenyl-methylene- group are removed, which results in the formation of alpha -ethynyl- 3,4-dihydroxy- phenylalanine. The alpha -vinyl- analog is obtained by hydrogenation of an intermediate. The compounds have a pharmaceutical activity.
IPC 1-7
IPC 8 full level
A61K 31/198 (2006.01); A61K 31/215 (2006.01); A61K 31/22 (2006.01); A61K 31/195 (2006.01); A61P 9/12 (2006.01); C07C 67/00 (2006.01); C07C 227/00 (2006.01); C07C 227/16 (2006.01); C07C 229/36 (2006.01); C07D 317/46 (2006.01); C07F 7/08 (2006.01)
CPC (source: EP US)
A61P 9/12 (2018.01 - EP); C07D 317/46 (2013.01 - EP US); C07F 7/0812 (2013.01 - EP US)
Citation (search report)
- FR 1850 M 19630610 - MERCK & CO INC [US]
- US 3132176 A 19640505 - BOLLINGER FREDERICK W, et al
Designated contracting state (EPC)
BE CH DE FR GB LU NL SE
DOCDB simple family (publication)
EP 0000035 A1 19781220; EP 0000035 B1 19820106; DE 2861499 D1 19820225; DK 240778 A 19790112; IE 47073 B1 19831214; IE 781079 L 19781201; IT 7849636 A0 19780531; JP S543036 A 19790111; US 4401676 A 19830830
DOCDB simple family (application)
EP 78100058 A 19780601; DE 2861499 T 19780601; DK 240778 A 19780531; IE 107978 A 19780530; IT 4963678 A 19780531; JP 6501778 A 19780601; US 80239077 A 19770601