PURPOSE: To obtain a new pivalic acid tetrazolyphenyl ester having elastase inhibitory activity and the therapeutic and preventive activity for pulmonary emphysema and endotoxin-induced pulmonary disorders, thus useful for pulmonary emphysema, interstitial pulmonary diseases, atherosclerosis, etc.
CONSTITUTION: The objective compound, a pivalic acid tetrazolylphenyl ester derivative of formula I [R1 is H, a lower alkyl, a di-lower alkylamino or a lower alkoxyl; R2 is H, a lower alkyl, a group of formula (CH2)k-R3 (R3 is amino, carboxyl or hydroxyl; (k) is an integar of 1-5), etc.] and salts thereof permissible as medicines, e.g. pivalic acid 2-(1H-tetrazol-5-yl)phenyl ester. This compound formula I can be obtained, for example, by esterification of a compound of formula II with a pivolayl halide in the presence of a tertiary amine (est. pref. pyridine) in an inert organic solvent (e.g. methylene chloride) at room temperature.
TAKAHASHI YOSHIKI
MORISONO DAISUKE
AGATA MITSUHARU
TOYOFUKU HATSUNORI
MAEDA MAKOTO
