Antiallergic 6-carboxy-2-cyclopropyl-chromone derivs. - also useful in antiulcer and bronchodilator medicaments

摘要

Chromone derivs. of formula (I) and their salts are new: In the formula, n=0 or 1; R1 is H or 1-20C alkyl opt. substd. by 2-5C alkanoyloxy or NR4R5; R4 and R5 are H or 1-10C alkyl, or NR4R5 is pyrrolidino, piperidino or morpholino; R2 is 1-8C alkyl or 3-4C alkenyl; R3 is an opt. Me-substd. furyl, thienyl or pyridyl gp., or a phenyl gp. opt. mono- or di-substd. by halogen and/or (O)mR8; m=0 or 1; R8 is 1-6C alkyl or 3-4C alkenyl opt. substd. by OH or 1-2C alkoxy. Cpds. (I) are anti-allergic agents, some with higher activity than Na cromoglycate. Cpds. (I) also have antiulcer and bronchodilatory activity. A typical cpd. (I) is trans-6-carboxy-3-propyl-2-(2-phenylcyclopropyl)-chromone. In an example, this is prepd. from methyl 3-valeroyl-4-hydroxybenzoate and trans-2-phenylcyclopropyl-1-carbonyl chloride.