摘要:
The invention relates to a method for the production of etoposide wherein 2,3 - diphenoxyacetyl -1-O-triethylsilyl -β-D- glucopyranoside is condensed with 4'-phenoxyacetyl-4'-demethylepipodophyllotoxine.
摘要:
The invention concerns a novel method for preparing mequitazine and its laevo-gyrate isomer, consisting in reacting the phenothiazine derivative containing lithium with 3-methane sulphonyl oxymethyl-1-aza-bicyclo(2,2,2)-octane or its laevo-gyrate isomer, in the presence of butyllithium.
摘要:
The invention pertains to novel azabicyclo-naphthalene-carboxamide derivatives, a method for preparing same and the use thereof as a medicament. The compounds of the invention are of formula (I).
摘要:
A novel method for preparing an optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative of general formula (II) is described, wherein R is a hydrogen atom, a halogen, a lower alkyl, lower alkoxy or hydroxy radical. The method comprises separating the racemic mixture by selective crystallisation with the suitable optically pure enantiomer of 2-phenylglycinol, in a suitable solvent, whereafter the optically pure, crystallised acid of formula (II) is isolated and recovered. The invention also provides the optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative thus obtained and the use thereof for the preparation of an optically pure derivative of efaroxan.
摘要:
The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamidc, or alkyl-urea or alkyl- sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: - R represents hydrogen or C 1-4 alkyI, - A represents CO(CH 2 ) n or CONH(CH 2 ) n where n = 2, 3, 4, or 5, - R1 and R2 are as described herein.
摘要:
The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.
摘要:
The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3- thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.
摘要:
A method for synthesising a 4'-demethylepipodophyllotoxin of formula (II) from a podophyllotoxin of formula (I) by treating it with a pair of reagents, i.e. a strong acid and an aliphatic, aromatic or functionalised sulphide, in the presence of an organic or inorganic acid, or in the presence of water with or without a water-miscible organic solvent.
摘要:
A compound of general formula (I), wherein R is a hydrogen atom, a straight or branched C1-4 alkyl radical or a straight or branched C1-4 alkoxy radical; and therapeutically acceptable salts, a racemic mixture or optically active isomers thereof; is used to prepare a drug for treating Parkinson's disease and its development.