| 摘要 |
This invention provides an improved process for producing methylene-cycloamines as exemplified by 1-isopropyl-3-diphenylmethyleneacetidine: <IMAGE> In accordance with the invention process, the above illustrated methyleneazetidine compound is synthesized by (1) reacting alpha , alpha -diphenyl- alpha -(1-isopropyl-3-azetidinyl) acetamide with bromine and alkali metal alkoxide under modified Hofmann Rearrangement conditions to form a carbamate intermediate, and (2) heating the carbamate intermediate in an acidic medium to yield the 1-isopropyl-3-diphenylmethyleneazetidine product. This illustrated 3-methyleneazetidine compound is characterized by a combination of pharmacological properties which are indicative of utility as a mood elevating therapeutic agent for relieving the symptoms of depression in humans. |
