摘要 |
<p>PURPOSE:To obtain the titled compound in short step, by reacting a compound such as 4-bromo-11-(2-tetrahydropyranyl)oxy-6,11-dihydrobenzo[b,e]oxepine with a metal, etc., and reacting the product with dialkyl carbonate. CONSTITUTION:The objective compound of formula II [one of R<5> and R<6> is COOR<8> (R<8> is H or alkyl) and the other is H; R<7> is H, alkyl, etc.] can be produced by reacting the compound of formula I (R<1> is alkyl or OH-protective group; one of R<2> and R<3> is halogen and the other is H; R<4> is H or alkyl) with an organometallic compound or a metal, and either by (i) reacting with di(lower alkyl) carbonate or lower alkyl halogenoformate, or (ii) reacting first with carbon dioxide and then with an acid, or (iii) reacting with carbon dioxide and then with an alkylation agent, and if necessary treating with an acid. EFFECT:The reaction proceeds under mild condition. USE:An antiallergic agent or its intermediate.</p> |