abstract |
PURPOSE: To obtain a new spiro dibenzosuberane derivative, capable of specifically antagonizing N-methyl-D-aspartic acid receptors, and useful as a medicine for cerebral dysfunction due to ischemia and an anticerebral neurocytotoxic agent for Alzheimer's disease, etc. n CONSTITUTION: A compound, e.g. spiro(dibenzosuberane-5,2'-pyrrolidine) expressed by formula I [R 1 is H, lower alkyl, lower alkenyl or aralkyl; R 2 is H or lower alkyl; R 3 and R 4 are H, lower alkyl, lower alkoxy or halogen; (m) is 0 or 1; (n) is 2-4]. The aforementioned compound is obtained by passing 5-cyanodibenzosuberane expressed by formula II as a starting substance through 5 steps, converting the above-mentioned compound into a compound expressed by formula III (Me is methyl) and treating the obtained compound expressed by formula III with a reducing agent (e.g. lithium aluminum hydride) in a suitable solvent (e.g. diethyl ether) at ambient temperature or while heating the above-mentioned reaction solution. n COPYRIGHT: (C)1992,JPO&Japio |