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.
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:
In the production of perparine or papaverine and their hydrochlorides, the formation of impurities in the reaction mixture is suppressed by fractionating a 3,4-di-R-benzyl-cyanide in the presence of an organic base (e.g. pyridine, dimethylformamide, ethylenediamine or triethylamine) followed by hydrogenation with a Raney-nickel catalyst treated with aqueous ammonium carbonate solution. R is methoxy or ethoxy.
摘要:
An inclusion complex is disclosed of N-(1-phenylethyl)-3, 3-diphenyl-propylamine or its hydrochloride complexed with a cyclodextrin as well as a process for the preparation thereof and pharmaceutical compositions containing same. The new inclusion complexes have coronary dilatory activity and have greater water soluble than simple N-(1-phenylethyl)-3, 3-diphenyl-propyl amine or the hydrochloride thereof.