摘要:
2-Aminothiophenol is reacted with methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, and the intermediate methyl (2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)propionate is cyclized in the presence of methanesulfonic acid, in the same vessel and without isolating said intermediate product, using e.g. chlorobenzene as a solvent.
摘要:
2-Aminothiophenol is reacted with (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl) methylpropionate, and the intermediate (2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl) methylpropionate is then cyclized in the presence of methane sulfonic acid, in the same container and without isolating said intermediate product, using chlorobenzene as a solvent.
摘要:
2-Aminothiophenol is reacted with methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, and the intermediate methyl (2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)propionate is cyclized in the presence of methanesulfonic acid, in the same vessel and without isolating said intermediate product, using e.g. chlorobenzene as a solvent.
摘要:
A process for the preparation of a methyl (+)-(2S,3S)-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)propionate of the formula (I): ##STR1## in which X denotes hydrogen or chlorine, which process comprises reacting a 2-aminothiophenol of formula (II): ##STR2## in which X is as defined above, with methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, in a 1,2-dichloroethane solvent.
摘要:
A process for the preparation of methyl (-)-(2R,3S)-2,3-epoxy-3-(4-methoxyphenyl)propionate, which comprises subjecting the dextrorotatory (2S,3R) enantiomer, present in a starting mixture containing both the levorotatory (2R,3S and dextrorotatory (2S,3R) enantiomers, to a transesterification reaction, in an anhydrous medium and in the presence of an enzyme which does not affect the levorotatory (2R,3S) enantiomer. The latter is an intermediate for the synthesis of compounds such as Diltiazem.
摘要:
Process for preparing diphenylazomethines of formula (II) ##STR1## by decarboxylation of diphenylazomethines of formula (I) ##STR2## in which X.sub.1 and X.sub.2 each denote, independently of each other, a hydrogen atom or a halogen atom or a methyl radical,R.sub.1 is H or linear or branched (C.sub.1-4) alkyl radical,R.sub.2 is the radical COOH, a linear or branched (C.sub.1-4) alkyl radical, the radical CONH.sub.2 or a linear or branched COO(C.sub.1-4) alkyl radical, andR.sub.3 denotes a hydrogen atom or the methyl radical.
摘要:
A pharmaceutical preparation intended for transdermal administration contains alfusozin [(N-[3-[(4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro-2-furancarboxamide] or a salt thereof and a mixture composed of water, at least one organic solvent and at least one absorption promoter.
摘要:
The present invention provides a piperidine derivative of formula (I) ##STR1## in which R represents a straight- or branched-chain (C.sub.1 -C.sub.19)alkyl group, a straight- or branched-chain (C.sub.2 -C.sub.19)alkenyl group, a (C.sub.3 -C.sub.6)cycloalkyl group, a cycloalkylmethyl group in which the cycloalkyl moiety has from three to six carbon atoms, a phenyl group which is optionally substituted by a halogen atom or a phenyl methyl group which is optionally substituted by a halogen atom, or an addition salt thereof, in the form of an optically pure enantiomer or of a mixture of enantiomers, a process for making them and their therapeutic application.
摘要:
Pharmaceutical compositions which comprises a core comprising alfuzosin hydrochloride which core is coated with a coating whose dissolution is pH-dependent and applications to the preparation of sustained-release dosage compositions which are unable for a once-daily oral administration.