| 摘要 |
<p>A process for producing 4-substituted-3-halogeno-1,4-benzoxazepine derivative or the salt thereof comprising: deprotonizing a benzoxazepine derivative having formula (II) with a base; and then, reacting the deprotonized product with a phosphate halide to produce an intermediate having formula (IV) and then, reacting the resultant intermediate (IV) with a reagent selected from (i) a complex of a phosphine with chlorine or bromine, (ii) a phosphine and a chlorine gas or liquid bromine, (iii) a phosphine and tetrachloromethane or tetrabromomethane, or (iv) a halogenated phosphite ester to product a 4-substituted-3-halogeno-1,4-benzoxazepine derivative having formula (I) wherein X indicates a chlorine atom or a bromine atom, or its salt.</p> |
