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 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:
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:
The invention relates to a novel process for preparing 1-[(2S)-3-mercapto-2-methyl-1-oxopropyl]-L-proline (captopril) of formula (I). ##STR1## which comprises hydrogenolysing 1-[(2S)-2-methyl-1-oxo-3-rhodanidopropyl]-L-proline of formula (II) ##STR2## in an inert solvent, in the presence of a catalyst, at a temperature of 50.degree. to 120.degree. C. under a pressure of 10.sup.5 to 10.sup.7 Pa.The above compound of formula (II) is new and can be prepared by acylating L-proline with a reactive acylating derivative of (2S)-2-methyl-3-rhodanido-propionic acid of formula (III). ##STR3##