Tocopheryl ester of 5-substituted picolinic acid, process for its production, and pharmaceutical composition containing it.

摘要

An a-tocopheryl 5-substituted picolinate of the formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="20" wi="82" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R represents an alkyl group which may have a substituent, a lower alkenyl group, a phenyl(lower alkyl) group, or a phenyl group which may have a substituent, and Q represents a methylene group or an oxygen or sulfur atom, or a pharmaceutically acceptable acid addition salt thereof. This compound can be produced by reacting a substituted picolinic acid of the formula
<Chemistry id="chema02" num="0002"><Image id="ia02" he="12" wi="35" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R and Q are as defined above, or its reactive derivative with a-tocopherol of the formula
<Chemistry id="chema03" num="0003"><Image id="ia03" he="23" wi="87" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>and as required, contacting the resulting compound with a pharmaceutically acceptable acid. A pharmaceutical composition comprising said compound as an active ingredient is useful for the treatment of hypertension.