PURPOSE: To prepare the titled compound useful as a remedy for coronary cardiopathy, in high yield, without producing by-product, by nitrating the 5-OH group of isosorbide having 2-OH group protected with stereo-selective protective group, and removing the protective group.

CONSTITUTION: Isosorbide protected with a stereo-selective protective group (e.g. triphenylmethyl) at the 2-OH group, is made to react with trityl chloride in a solvent such as pyridine at a temperature between 80°C and the boiling point of the solvent for 1W2hr to obtain 2-o-trityl-isosorbide of formulaI, which is converted to 2-o-trityl-isosorbide-5-nitrate of formula II by the nitration with a nitrating agent (e.g. a mixture of nitric acid, acetic anhydride and acetic acid) at ≤10°C for 1W2hr. The objective compound can be obtained by treating the above product with an acid in a solvent such as ether, thereby removing the protective group.