摘要:
Process for the synthesis of racemic thioctic acid comprising the following stages: a) reaction of the alkyl ester of 6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis selected from the group consisting of quaternary ammonium or phosphonium salts having the following general formula: where: A is nitrogen of phosphorus, X is selected from the group consisting of Cl, Br, I, HSO4, and H2PO4 and the substitutents R1, R2, R3 and R4 are selection from the group consisting of linear or branched alkyl radicals having one to twenty carbon atoms (C1-C20), said substituents being identical or different one from the other, or only one of said substituents is selected from the group consisting of arylalkyl radicals having the following formula —(CH2)nC6H5 in which n=1-16; b) followed by the hydrolysis of the ester of racemic thiotic acid.
摘要翻译:包括以下步骤合成外消旋硫辛酸的方法:a)在相转移化合物存在下,6,8-二卤代辛酸的烷基酯在有机溶剂中与碱性二硫化物水溶液的反应 选自具有以下通式的季铵或鏻盐的催化剂:其中:A是磷的氮,X选自Cl,Br,I,HSO 4和H 2 PO 4,取代基R1,R2 ,R3和R4选自具有1-20个碳原子的直链或支链烷基(C1-C20),所述取代基彼此相同或不同,或者只有一个所述取代基选自基团 由具有下式的芳基烷基 - (CH 2)n C 6 H 5,其中n = 1-16; b)然后水解外消旋硫酸的酯。
摘要:
The invention concerns a new process for the preparation of naphthoquinones, in particular an improved process for the preparation of 2,3-disubstituted 1,4-naphthoquinones, in the trans configuration.
摘要:
The invention concerns a new process for the preparation of high purity diacerein, by oxidization of the protected aloe-emodin in the presence of an oxidizing system and radical catalyst and subsequent substitution of the protector groups with acetyl groups.
摘要:
The invention concerns a new process for the preparation of naphthoquinones, in particular an improved process for the preparation of 2,3-disubstituted 1,4-naphthoquinones, in the trans configuration.
摘要:
The invention concerns a new process for the preparation of high purity diacerein, by oxidisation of the protected aloe-emodin in the presence of an oxidising system and radical catalyst and subsequent substitution of the protector groups with acetyl groups.
摘要:
A process for preparing pyrido-benzothiazine derivatives having the following general formula: ##STR1## in which R is H or a C.sub.1 -C.sub.6 alkyl or a C.sub.1 -C.sub.6 fluoroalkyl, and R.sub.1 is N-alkyl-3-pyrrolidinalkylamine with C.sub.1 to C.sub.6 alkyls or ##STR2## where R.sub.2 is a C.sub.1 -C.sub.6 alkyl or a C.sub.2 -C.sub.6 alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form. The process for the preparation of derivatives of formula (I) starts with a first reaction cycle starting from 2,4-difluoro-3-chloronitrobenzene. Said derivatives possess a high antibacterial activity as well as a high bioavailability to tissues. The invention also refers to pharmaceutical compositions containing them as active components.
摘要:
Pyrido-benzothiazine derivatives having the following general formula: ##STR1## in which R is H or a C.sub.1 -C.sub.6 alkyl or a C.sub.1 -C.sub.6 fluoroalkyl, and R.sub.1 is N-alkyl-3-pyrrolidinalkylamine with C.sub.1 to C.sub.6 alkyls or ##STR2## where R.sub.2 is a S.sub.1 -C.sub.6 alkyl or a C.sub.2 -C.sub.6 alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form.The invention also comprises the process for the preparation of derivatives of formula (I) starting from 2.4-difluoro-3-chloronitrobenzene.Said derivatives possess a high antibacterial acitvity as well as a high bioavailability to tissues; the invention also refers to pharmaceutical compositions containing them as active components.
摘要:
New 1,5-benzothiazepines of the following general formula ##STR1## wherein: R.sub.1 represents (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy or a halogen atom;R.sub.2 is selected from: benzoyl independently substituted with 1 to 3 (C.sub.1-4)alkyl or (C.sub.1-4)alkoxy groups, or with halogen atoms; phenylcarbamoyl; phenylcarbamoyl independently substituted with 1 to 3 (C.sub.1-4) alkyl or (C.sub.1-4) alkoxy groups or with halogen atoms; the groups R.sub.5 -CO, in which R.sub.5 is the radical deriving from a heterocyclic ring optionally substituted by a (C.sub.1-4)alkyl or a (C.sub.1-4)alkoxy radical, or by a halogen atom;R.sub.3 and R.sub.4 independently represent (C.sub.1-4)alkyl groups; and salts therewith of pharmaceutically acceptable acids.The compounds of the invention possess cardiovascular utility.
摘要:
The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
摘要:
The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.