| 摘要 |
<p>The invention comprises compounds of formula <FORM:1040162/C2/1> in which R1 is a cycloalkylmethyl group and R2 is a halogen atom, and the preparation of substituted 1,4-benzodiazepines of formula <FORM:1040162/C2/2> by reacting a 2-(N-phthalimidoacetyl-N-cycloalkylmethyl) - amino - 5 - halobenzophenone of Formula I above with hydrazine hydrate. The 2 - (N - phthalimidoacetyl - N - cycloalkylmethyl). amino-5-halobenzophenone is prepared by treating a 2-amino-5-halobenzophenone dissolved in a mixture of tetrahydrofuran and triethylamine with an equal molar ratio of the desired cycloalkane-carboxylic acid chloride, treating the 2 - cycloalkylcarbonylamino - 5- halobenzophenone formed with an alkali metal complex hydride, e.g. lithium aluminium hydride, followed by aqueous hydrolysis to yield the corresponding 2 - cycloalkylmethylamino - 5 - halobenzhydrol, oxidizing this compound with an excess of manganese dioxide to give 2-cycloalkylmethylamino-5-halobenzophenone which is reacted with phthalimido-acetyl chloride in tetrahydrofuran.</p> |
