摘要:
3-Phenoxybenzene derivatives are prepared by a method which comprises the steps of(a) chlorinating benzaldehyde with chlorine gas in the presence of a hydrocarbon and a Lewis acid catalyst to obtain 3-chlorobenzaldehyde; (b) reacting the 3-chlorobenzaldehyde with ethylene glycol to obtain 2-(3-chlorophenyl)-1,3-dioxolane; (c) etherifying said dioxolane with an alkali phenolate to yield the intermediate 2-(3-phenoxyphenyl)-1,3-dioxolane and converting this intermediate to the corresponding aldehyde, cyanohydrin, sulfonic acid salt or oxime derivative.
摘要:
2-(3-Phenoxy-phenyl)-propionic acid or its pharmaceutical treatments, are prepared by hydrolyzing and partially decarboxylating ##STR1## wherein R=C.sub.1 -C.sub.6 alkyl or amino, the latter compounds being themselves new and, where R=C.sub.1 -C.sub.6 alkyl, have antiinflammatory pharmaceutical properties.
摘要:
The invention relates to a process for the preparation of compounds of formula (I) ##STR1## wherein R.sup.1 stands for hydrogen or the group COR.sup.2, whereinR.sup.2 stands for a straight or branched chained alkyl having 1 to 8 carbon atoms optionally substituted with phenyl, naphthyl, tetrahydronaphthyl or m-phenoxy-benzyl, cycloalkyl having 3 to 6 carbon atoms optionally substituted with one or more straight or branched chained alkyl or alkenyl having 1 to 6 carbon atoms, phenyl or naphthyl.The compounds of formula (I) are prepared according to the invention by(a) reacting esters of formula (II) ##STR2## wherein X stands for chlorine or bromine andR.sup.2 has the same meanings as defined above with a phenol alkali metal salt and(b) if desired converting the diphenyl ethers so obtained to a specific compound of formula (I), m-phenoxybenzyl alcohol by the hydrolysis of the ester group.
摘要:
2-(3-phenoxy-phenyl)-propionic acid or its pharmaceutical treatments, are prepared by hydrolyzing and partially decarboxylating ##STR1## wherein R=C.sub.1 -C.sub.6 alkyl or amino, the latter compounds being themselves new and, where R=C.sub.1 -C.sub.6 alkyl, have antiinflammatory pharmaceutical properties.
摘要:
A process for the preparation of anthelmintic compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen or --COOR;R.sup.5 is C.sub.1 to C.sub.4 alkyl;R.sup.2 is halogen, alkyl, trifluoromethyl, alkoxy, aryloxy, or aralkoxy; andR.sup.4 is hydrogen, alkyl, cycloalkyl; alkenyl, alkynyl or aralkyl;or pharmaceutically acceptable salts thereof comprises subjecting a bis compound of the formula: ##STR2## to reduction to cleave the disulfide linkage and where R.sup.4 is other then hydrogen, subsequent reaction of the mercapto group. Intermediate compounds and a process for preparing same are also disclosed.
摘要:
A process is described for the preparation of 4-Methyl-5-(2-Chloroalkyl)-thiazole wherein the alkyl ranges from C.sub.2 -C.sub.5, by providing the steps of either a) converting the 3-thiocyanato-5-chloro-2-alkanone into 2-chloro-4-methyl-5-(2-chloroalkyl)-thiazole by gaseous hydrochloric acid in an organic solvent and hydrogenating the compound in the presence of a metal catalyst in an organic solvent, or b) reacting 3-thiocyanato-5-choro-2-alkanone with aqueous mineral acid and treating the thiazole obtained with a halogenating agent, and hydrogenating the 2-chloro-4-methyl-5-(2-chloroalkyl)-thiazole in an organic solvent in presence of a metal catalyst.
摘要:
The present invention relates to a process for the preparation of compounds of general formula (I), wherein R stands for a straight chained C.sub.1-5 alkyl group substituted by a chlorine atom in the 2-position, and acid addition salts thereof, characterized by reacting a 3,5-dichloro-2-alkanone of general formula (V), wherein R is a defined above, with an inorganic thiocyamate, and a) converting the 3-thiocyanato-5-chloro-2-alkanone of general formula (IV), thus obtained, wherein R is as defined above, into 2-chloro-4-methyl-5-(2-chloroalkyl)-thiazole of general formula (II), wherein R is as defined above, by gaseous hydrochloric acid in an organic solvent, hydrogenating the said compound in the presence of a metal catalyst in an organic solvent, or b) reacting said compound of general formula (IV) with an aqueous mineral acid and treating the 2-hydroxy-4-methyl-5-(2-chloroalkyl)-thiazole of general formula (III), thus obtained with a halogenating agent, and hydrogenating the 2-chloro-4-methyl-5-(2-chloroalkyl)-thiazole of general formula (II) thus obtained, wherein R is as defined above, in an organic solvent in presence of a metal catalyst, and optionally converting the 4-methyl-5-(2-chloroalkyl)-thiazole of general formula (I), wherein R is as defined above, thus obtained or a hydrochloride salt thereof, in a manner known per into another acid addition salt or setting free a compound of general formula (I), wherein R is a defined above, from its acid addition salt.
摘要:
Antitussive compounds of the formula I ##STR1## or physiologically acceptable acid addition salts thereof are disclosed, where A stands for straight or branched chain C.sub.1-5 alkylene or ##STR2## R.sub.1 stands for straight or branched chain C.sub.1-10 alkyl, halogenoalkyl, hydroxyalkyl, C.sub.5-6 cycloalkyl, vinyl, 2-ethoxyethyl, carbonylalkyl or aminoalkyl of the formula ##STR3## wherein R stands for hydrogen or methyl, n is 0 to 3,R.sub.2 stands for hydrogen or straight or branched chain alkyl,R.sub.3 stands for hydrogen or straight or branched chain alkyl or,R.sub.2 and R.sub.3 together with the nitrogen atom may form a 5-6 membered ring, which ring can optionally contain an oxygen or a second nitrogen atom, the latter, optionally substituted by methyl or,R.sub.1 can stand for a phenyl group of the formulaR.sub.4 R.sub.5 C.sub.6 H.sub.3 whereinR.sub.4 and R.sub.5 represent independently hydrogen, chlorine, hydroxy, methoxy, ethoxy, methyl or amino or,R.sub.1 may further stand for hydroxy, in this case the compound of the formula I may exist according to the conditions in the form of tautomers of the formula Ia ##STR4## and R.sub.1 may further stand for benzyl, 2,2-diphenylethyl or theophyllin-7-yl-methyl.
摘要:
Arylacetic acid derivatives of the formula ##STR1## with R.sup.1, R.sup.2 and R.sup.3 specifically defined and which are useful as antirheumatic and antiinflammatory pharmaceuticals are prepared by catalytic hydrogenation of new compounds of the formula ##STR2## in which R and R.sup.10 are also specifically defined. The method of making the latter compound is also set forth.
摘要:
Arylacetic acid derivatives of the formula ##STR1## with R.sup.1, R.sup.2 and R.sup.3 specifically defined and which are useful as antirheumatic and antiinflammatory pharmaceuticals are practiced by catalytic hydrogenation of new compounds of the formula ##STR2## in which R and R.sup.10 are also specifically defined. The method of making the latter compound is also set forth.