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:
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:
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.
摘要:
New compounds of the formula (VIIIa) are disclosed ##STR1## wherein R.sup.1 is hydrogen, methyl or ethyl;R.sup.2 is hydrogen, fluoro, or alkyl having 1 to 4 carbon atoms;R.sup.3 is hydrogen, phenyl, alkoxy having 1 to 6 carbon atoms; phenoxy, thenoyl, or benzoyl; orR.sup.2 and R.sup.3 together with the phenyl group to which they are attached form a naphthyl group which is unsubstituted or substituted by C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy;R.sup.10 is phenylaminocarbonyl, 1-phenyl-5-tetrazolyl, a group --SO.sub.2 OMe, wherein Me is a metal atom selected from the group which consists of sodium or potassium, or a group --SO.sub.2 R.sup.6 in which R.sup.6 is alkyl having 1 to 4 carbon atoms, 4-methylphenyl, amino, C.sub.1 to C.sub.4 alkoxycarbonyl-amino, or benzoylamino, or R.sup.10 is a group ##STR2## in which R.sup.7 is cycloalkyl having 5 to 6 carbon atoms, and R is vinyl. The compounds are intermediates useful in the preparation of arylacetic acids having antiinflammatory compounds.
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:
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:
A new process is disclosed for the preparation of a compound of the formula (VIII) ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-3 alkoxy, or trifluoromethyl;R.sup.5 is amino or C.sub.1-4 alkoxycarbonylamino; or a salt thereof, which comprises reacting a compound of the formula (II) ##STR2## with gaseous chlorine and a rhodanide of the formula (III)R--SCN (III)wherein R represents a metal ion or ammonium.
摘要:
A process is disclosed for the preparation of a compound of the formula (XI) ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen, halogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.3 alkoxy, or trifluoromethyl;R.sup.5 is amino or C.sub.1 to C.sub.4 alkoxycarbonylamino; andR.sup.4" is C.sub.1 to C.sub.6 alkyl, C.sub.2 to C.sub.6 alkenyl, C.sub.2 to C.sub.6 alkynyl, cyclohexyl, benzyl, or 2-phenyl-ethyl, which comprises the steps of:(a) reacting a compound of the formula (VIII) ##STR2## or a salt thereof, with a basic nucleophilic compound to yield a salt of the formula (IX) ##STR3## wherein R.sup.4' is a lone pair of electrons, in which case an alkali metal or alkali earth metal cation forms a salt with the sulfur atom; and(b) reacting a salt of the formula (IX) with a compound of the formula (X)R.sup.4' --QwhereinQ is hydroxyl, halogen, 1/2SO.sub.4, 1/3PO.sub.3, SO.sub.3 C.sub.6 H.sub.5, or SO.sub.3 C.sub.6 H.sub.4 CH.sub.3 to yield the desired product.
摘要翻译:公开了制备式(XI)化合物或其盐的方法,其中R 1是氢,卤素,C 1至C 4烷基,C 1至C 3烷氧基或三氟甲基; R5是氨基或C1-C4烷氧基羰基氨基; 并且R 4“为C 1至C 6烷基,C 2至C 6烯基,C 2至C 6炔基,环己基,苄基或2-苯基 - 乙基,其包括以下步骤:(a)使式(Ⅷ) IMAGE>或其盐与碱性亲核性化合物反应得到式(Ⅸ)的盐,其中R4'是一对电子,在这种情况下,碱金属或碱土金属阳离子与 硫原子; 和(b)使式(IX)的盐与式(X)R4'-Q的化合物反应,其中Q是羟基,卤素,1 / 2SO 4,1 / 3PO 3,SO 3 C 6 H 5或SO 3 C 6 H 4 CH 3,得到所需产物 。