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:
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 。
摘要:
The present invention relates to novel compounds of the general formula ##STR1## wherein R is hydrogen atom or a trifluoromethyl, carboxy, C.sub.2-5 alkoxycarbonyl, cyano, benzoyl, sulfamoyl or C.sub.1-4 alkylsulfonyl group;R.sup.1 is hydrogen atom or a linear or branched chain C.sub.1-4 alkyl, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfonyl, benzylthio, benzylsulfonyl, phenyl, hydroxy or mercapto group; andR.sup.2 is hydrogen or chlorine atom,as well as their pharmaceutically acceptable salts.The compounds according to the invention possess diuretic and saluretic activity with an advantageous Na/K ratio.
摘要:
Diuretic and saluretic tetrahydro-isoquinoline derivatives of the Formula (I) ##STR1## wherein R stands for hydrogen or chlorine,R.sup.1 and R.sup.2 are hydrogen, methoxy or ethoxy, andR.sup.3 and R.sup.4 are hydrogen or methyl,and a process for the preparation thereof as well as pharmaceutical compositions containing as active ingredients isoquinoline derivatives of the Formula (I). The compounds of Formula I are prepared by reacting a 2-amino-tetrahydro-isoquinoline derivative of the Formula (II) ##STR2## with a carboxylic acid derivative of the Formula (III) ##STR3## wherein x stands for chlorine, --OH, --OCH.sub.2 CN, --OCH.sub.3, --OC.sub.2 H.sub.5, --OCOOCH.sub.3 or --OCOOC.sub.2 H.sub.5R.sup.5 and R.sup.6 stand for hydrogen or together from CHN(CH.sub.3).sub.2 and in case of the Formula (Ia) ##STR4## splitting off the protective group in alkaline medium.