| 摘要 |
<p>PCT No. PCT/JP98/03153 Sec. 371 Date Nov. 24, 1999 Sec. 102(e) Date Nov. 24, 1999 PCT Filed Jul. 14, 1998 PCT Pub. No. WO99/03847 PCT Pub. Date Jan. 28, 1999A process for producing 4-substituted-3-halogeno-1,4-benzoxazepin derivative or the salt thereof comprising: deprotonizing a benzoxazepine derivative having the formula (II): with a base; and then, reacting the deprotonized product with a phosphate halide to produce an intermediate having the 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 produce a 4-substituted-3-halogeno-1,4-benzoxazepine derivative having the formula (I) wherein X indicates a chlorine atom or a bromine atom, or its salt.</p> |
