| 摘要 |
<p>NEW MATERIAL:A compound of formulaI(R and R<2> are H or lower alkyl; R<1> is acyl; the dotted line is single or double bond). EXAMPLE:Methyl 5-acetyl-5,6-dihydro-1H-azepino[5,4,3-cd]indole-4-carboxylate. USE:A synthetic intermediate for various indole alkaloids having coronary arterial vasodilator action. PROCESS:One mole compound of formula II (R' is protecting group or lower alkyl; R<1> is acyl; R<2>' is lower alkyl; X is eliminative group) is subjected to the ring closing reaction with 0.1-10mol acid, e.g. formic or acetic acid, preferably in the presence of an acid anhydride, e.g. acetic or propionic anhydride, at room temperature -120 deg.C, and then the removal of the protecting group, hydrolysis or/and reduction treatment if necessary to give the compound of formulaI. The starting raw material compound of formula II is obtained by reacting a compound of formula III with a compound of formula IV.</p> |
