PURPOSE: To obtain a new cyclopropyl derivative useful for treating or relieving inflammatory, allergic and cardiovascular diseases for humans as the object in addition to inhibition to lipoxygenase enzyme.
CONSTITUTION: A compound expressed by formula I {A is 1-3C alkylene; Ar is phenyl or styryl; A is alkyl halide or NHR' (R' is alkylthioalkyl or H and Ar is styryl when R' is H) or formula II [(n) is 1-4; (p) is 2-5]} and its pharmaceutically permissible salt, e.g. N-hydroxy-N-[(2-trans-styrylcyclopropyl) methyl]urea. The compound expressed by formula I is obtained by reducing a ketone derivative of cyclopropane expressed by formula III (Q is formula IV), providing an alcohol expressed by formula V, treating the resultant alcohol expressed by formula V with N,O-bis(tert-butoxycarbonyl)hydroxylamine under conditions of the MITSUNOBU type reaction, then carrying out acid catalyzed hydrolysis of the N,O-protected intermediate product and reacting the prepared hydroxylamine expressed by formula VI with the corresponding substituted acetyl chloride or a suitable isocyanate.
IKEDA TAKAFUMI
RODONII UIRIAMU SUTEIIBUNSU
MANO TAKASHI
OKUMURA YOSHIMASA
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