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:
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:
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:
The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.
摘要:
The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.
摘要:
The invention relates to a method of treating or preventing illnesses resulting from damaged endothelial cells, wherein the method comprises administering to a patient a product comprising hydroxylamine derivatives of the general formulae (I) ##STR1## with the proviso that in the compounds of general formula (I) when X comprises a --NR.sup.3 R.sup.4 group and Y comprises a hydroxyl group, the X group is condensed with the Y substituent to form an intramolecular ring represented by general formula (Ill) ##STR2##
摘要:
Hydroximic acid derivatives possess anti-ischemic effects, and therefore, they are useful for treating ischemic states and diseases, such as myocardial ischemia (which may be induced by occlusion of coronary arteries). These derivatives include compounds of formula (I): ##STR1## wherein: X represents a halogen; Z represents an aromatic group, a pyridinyl group, a picolyl group, or a lutidyl group; and R represents an --A--N(R.sub.1)R.sub.2 group, wherein:R.sub.1 and R.sub.2 represent, independently from each other, hydrogen or an alkyl group;or R.sub.1 and R.sub.2, together with the adjacent nitrogen atom, form a 5- to 7-membered,saturated heterocyclic group optionally containing an additional nitrogen, oxygen,or sulfur atom, the heterocyclic group optionally being substituted by at least one alkyl group; andA represents a straight or branched chain alkylene group, as well as pharmaceutically acceptable acid addition salts thereof. The invention further relates to processes for preparing the above noted compounds, and pharmaceutical compositions containing these compounds or their pharmaceutically acceptable acid addition salts as an active ingredient. Additionally, the invention relates to intermediate compounds of formula II used in preparing the compounds of formula I. Formula II is as follows: ##STR2## In formula II, the variables Z and R have the same definitions provided above.
摘要:
The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions containing the carboxamidine derivatives of the invention, and the use thereof for the treatment of vascular diseases and in the preparation of pharmaceutical compositions for the treatment of vascular diseases.
摘要:
The subject invention relates to carboxamidine derivatives, to pharmaceutical compositions comprising the same, and the use thereof in the preparation of pharmaceutical compositions for the treatment of vascular diseases.
摘要:
The invention relates to carboxamidine derivatives to pharmaceutical compositions containing the same and the use thereof in the preparation of pharmaceutical compositions for the treatment of vascular diseases.