摘要:
This invention relates to a process for the preparation of 7-hydroxy taxanes of general formula (I) from 7-trialkylsilyl taxanes of general formula (II), wherein R.sub.1 is hydrogen, alkoxy, acyloxy, or alkoxyacetoxy, and Z is a hydrogen atom or a radical of general formula (III), wherein R.sub.2 is an optionally substituted benzyl radical or an R'.sub.2 --O--CO-- radical wherein R'.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical, R.sub.3 is an aromatic alkyl, alkenyl, alkynyl, cycloalyl, phenyl, naphthyl or heterocyclyl radical and either R.sub.4 is a hydrogen atom and R.sub.5 is a hydroxyl function protecting group, or R.sub.4 and R.sub.5 together form a saturated 5- or 6-membered heterocylic ring. In general formula (II), each R, which are the same or different, is an alkyl radical optionally substituted by a phenyl radical. ##STR1##
摘要:
The present invention relates to a novel process for the preparation of 7-trialkylsilylbaccatin III of general formula: ##STR1## in which the symbols R, which may be identical or different, represent alkyl radicals containing 1 to 4 carbon atoms which are optionally substituted with a phenyl radical, starting with 10-deacetylbaccatin III of formula: ##STR2## In the general formula (I), each of the symbols R preferably represents a straight or branched alkyl radical containing 1 to 4 carbon atoms. Even more particularly, each of the symbols R represents an ethyl radical.
摘要:
Group A streptogramin derivatives of general formula (I) in which: R1 represents a halogen atom or an azido or thiocyanato radical, R2 represents a hydrogen atom or a methyl or ethyl radical, R3 represents a hydrogen atom, or the residue of an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclylaliphatic ester which may be substituted, and the bond --- represents a single bond (stereochemistry 27R) or a double bond, as well as its salts when they exist
摘要:
The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR′R″ in which R′ and R″ represent an alkyl, a hydrogen or an amino-protecting group; c) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.
摘要:
Group A streptogramin derivatives of general formula (I) in which: R1 represents a halogen atom or an azido or thiocyanato radical, R2 represents a hydrogen atom or a methyl or ethyl radical, R3 represents a hydrogen atom, or the residue of an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclylaliphatic ester which may be substituted, and the bond - - - represents a single bond (stereochemistry 27R) or a double bond, as well as its salts when they exist.
摘要:
The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR′R″ in which R′ and R″ represent an alkyl, a hydrogen or an amino-protecting group; c) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.
摘要:
A cyclosporin compound of the formula (I): ##STR1## wherein Alk and R are as defined herein, or a pharmaceutically acceptable salt thereof, which derivatives are is useful in the treatment and/or prophylaxis of retrovirus infections.