Document Type and Number:
Japanese Patent JPS5318022
Kind Code:
B2
Abstract:
1389984 Sulphuric and phosphoric esters of substituted carvacrols WARNER-LAMBERT CO 30 July 1973 [3 Aug 1972] 36153/73 Headings C2P and C2C The invention comprises esters of the general formula wherein R 1 is H or C 1 -C 5 alkyl, R 2 is H or C 1 -C 5 alkyl and R 3 is a sulphuric or phosphoric acid residue which latter may be esterified with 1 or 2 further carvacryl residues present in the given formula, and the alkali metal salts of acidic sulphuric and phosphoric acid esters and the salts of sulphuric and phosphoric acid esters with pharmaceutically compatible acids. They may be obtained by reacting the corresponding carvacrol derivatives either with sulphamic acid or chlorsulphonic acid in the presence of a tertiary amine to give the sulphuric acid esters or with POCl 3 , using appropriate molar proportions to form the triester or the phosphoric acid ester mono- or di-halide, and then hydrolysing or saponifying the ester halides to give the mono- or bis-ester or the salts thereof. The compounds are useful as peripheral dilators and may be used in admixture with a solid or liquid pharmaceutically acceptable diluent or carrier. Compounds of the general formula wherein R 1 is H or C 1 -C 5 alkyl and R 2 is H are stated to be novel and can be obtained by cyanogen bromide degradation of the corresponding dialkylamino compounds a detailed example being given for the production of 4-(2-methylaminoethoxy)-carvacrol by this process, the product being isolated in the form of its hydrochloride.
Application Number:
JP8692673A
Publication Date:
June 13, 1978
Filing Date:
August 03, 1973
Export Citation:
International Classes:
A61K31/255; A61K31/66; A61P9/08; C07C67/00; C07C301/00; C07C303/24; C07C305/22; C07C305/24; C07F9/12; (IPC1-7): C07C141/16; A61K31/255; A61K31/66; C07C139/10; C07F9/12