摘要:
The invention relates to a new process for preparing known thiolcarbamate esters of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 stand independently for hydrogen or a straight or branched chain alkyl group containing 1 to 6 carbon atoms or an alkenyl group containing 2 to 6 atoms, or an alkyl group containing 1 to 6 or an alkenyl group containing 2 to 6 carbon atoms and mono- or polysubstituted by halogen, oxygen, sulphur and/or nitrogen; orR.sup.1 and R.sup.2 together may represent an optionally substituted .alpha.,.omega.-alkylene group containing 4 to 6 carbon atoms;R.sup.3 and R.sup.4 stand independently for hydrogen or an alkyl group containing 1 to 4 carbon atoms and optionally substituted by halogen or by a group containing oxygen, sulphur and/or nitrogen; andR.sup.5 and R.sup.6 both stand for hydrogen; orR.sup.5 and R.sup.6 together may represent a chemical bond.The compounds of general formula (I) are prepared by reacting(a) thiolcarbamate salts of the general formula (II) ##STR2## wherein the meanings of R.sup.1 and R.sup.2 are as defined above, andY stands for a primary, secondary or tertiary ammonium ion or an alkaline metal ion; or(b) amines of the general formula (III) ##STR3## wherein the meanings of R.sup.1 and R.sup.2 are as defined above, together with sulphur and carbon monoxide; or(c) amine of the general formula (III) together with carbonyl sulphidewith alkynes of the general formula (IV)R.sup.3 --C.tbd.C--R.sup.4 (IV)wherein the meanings of R.sup.3 and R.sup.4 are as defined above and, if desired, hydrogenating the obtained product of general formula (I), wherein the meanings of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above and R.sup.5 together with R.sup.6 forms a chemical bond, to a compound of the general formula (I), wherein both R.sup.5 and R.sup.6 stand for hydrogen.
摘要:
The invention relates to a process for preparing arylsulphonyl isocyanates of the general formula (I) ##STR1## and addition derivatives thereof--where in the formula the meaning of the substituents are as follows:Ar represents optionally substituted aryl, naphthyl- or thienyl group, andHX is a chemical bond or XZR.sub.1 stands for a group where Z is oxygen or sulphur,R.sub.1 is saturated or unsaturated alkyl, benzyl, cyclohexyl or substituted phenyl group orX is an NR.sub.2 R.sub.3 groupwherein R.sub.2 R.sub.3 is hydrogen, alkyl, unsubstituted alkyl, aryl, substituted aryl, aroyl or acyl group, and the essence of the process is that an N-halogen sulphonamidate is carbonylated in the presence of a carbonylating catalyst, in the presence or absence of alcohol, (thio) alcohol or amine reactants and the carbonylated compound obtained is reacted subsequently with the reactants.
摘要:
The invention relates to a process for the preparation of tetracycline derivatives of the formula ##STR1## and acid addition salts thereof --wherein R stands for --CH.sub.3 or .dbd.CH.sub.2 --by dehalogenating and hydrogenating chloromethacycline or acid addition salt thereof of the formula ##STR2## or by hydrating methacycline or acid addition salts thereof of the formula ##STR3## by treatment with hydrogen gas in the presence of a noble metal alloy catalyst on carrier and organic solvent which comprises performing, hydrogenating under pressure of 0.1-1.0 MPa with an alloy catalyst consisting of the alloy palladium or platinum and selenium and/or tellurium used at a ratio of 1:0.01-0.5 related to the amount of the starting tetracycline and carrying out, if desired dehalogenation and hydrogenation in one step.
摘要:
The invention relates to a process for preparing sulphonyl-ureas of the general formula (I) ##STR1## wherein Ar.sub.1 represents a phenyl, naphthyl or thienyl group, the derivatives thereof substituted by C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (halo)alkoxycarbonyl, (halo)alkyloxy, nitro, cyano groups as well as by halogen atoms,Ar.sub.2 represents a phenyl, pyridyl, pirimidinyl or triazinyl group and the derivatives thereof substituted by C.sub.1-4 (halo)alkyl, C.sub.1-4 (halo)alkyloxy, amino, O-acyl, O-arylsulphonyl, O-(substituted carbamoyl) groups as well as by halogen atoms.According to the invention N-halogen aryl sulphonamidate is reacted in the presence of a carbonylating catalyst, carbon monoxide and an aromatic amine, optionally in the presence of a phase transfer catalyst, or N-halogen aryl sulphonamidate is reacted with carbon monoxide in the presence of a carbonylating catalyst, and optionally in the presence of a phase transfer catalyst, then the obtained reaction mixture is further reacted with an aromatic amine or an N-halogen-arylamine-alkali metal salt is reacted with aryl-sulphonamid in the presence of a carbonylating catalyst, carbon monoxide and optionally in the presence of a phase transfer catalyst or an amine, amine dihalogenid, aryl sulphonamid are reacted in the presence of a carbonylating catalyst and carbon monoxide and the obtained reaction mixture is worked up in a known manner.The thus prepared sulphonyl-ureas are biologically active compounds, which are used in the pharmaceutical industry and for regulating plant growth.
摘要:
A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom may form a saturated or unsaturated heterocycle, or a condensed and/or substituted ring system, and said heterocycle or said condensed and/or substituted ring system may contain also a sulfo group,can be manufactured by reacting an amine of formula (II) ##STR2## with an N-carbamoyl-benzoic acid sulfimide derivative of formula (III) ##STR3## The disclosed N-acylating composition comprises of from 3 to 60% by weight, preferably of from 5 to 50% by weight sulfimide derivative of formula (III), of from 97 to 40% by weight, preferably of from 95 to 50% by weight solvent, and if desired, an organic or inorganic base.The disclosed N-acylating concentrate comprises of from 60 to 95.5% by weight N-acylating agent of formula (III) and of from 4.5 to 40% by weight additives.
摘要:
A process is disclosed for preparing a carbamic acid phenyl ester of the formula (I) ##STR1## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, or aralkyl having 7 to 16 carbon atoms, wherein the aryl, cycloalkyl or aralkyl is unsubstituted or substituted by at least one alkyl group having 1 to 8 carbon atoms;R.sub.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, cyanomethyl, 1,3-dioxolan-2-yl, or carboalkoxyamino wherein the alkoxy group contains 1 to 4 carbon atoms;R.sub.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms; orR.sub.1 and R.sub.2 form together a carbocyclic ring or a heterocyclic ring fused to the phenyl ring wherein the carbocyclic ring of the heterocyclic ring is unsubstituted or substituted by at least one alkyl having 1 to 8 carbon atoms, which comprises acylating a phenol of the formula (II) ##STR2## with a compound of the formula (IV) ##STR3## in the presence of a base. The compounds obtained are valuable intermediates.
摘要:
The invention relates to a process for the preparation of carbamic acid phenyl esters of the formula (I) ##STR1## by acylating phenol derivatives of the formula (II) ##STR2## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, aralkyl having 7 to 16 carbon atoms which groups can be substituted by one or more alkyl groups,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms or acylamino,R.sup.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, or ifR.sup.1 and R.sup.2 represent alkyl and/or alkoxy, they can form together a carbocyclic ring.According to the invention the phenol derivatives of the general formula (II), wherein R.sup.1 and R.sup.2 are as defined above, are reacted with N-carbamoyl-saccharin derivatives of the formula (IV) ##STR3## wherein R has the same meaning as defined above, in the presence of a base.