| 摘要 |
<p>There is disclosed a process for the preparation of 5-substituted-1-azabicycloÄ3.3.0Üoctanes of the Formula <CHEM> wherein R<1> is a cyano radical or group of -CO2R<3>, in which R<3> is a lower alkyl group. The derivative is prepared by reacting 1,7-disubstituted-4-heptanone of the Formula <CHEM> wherein X is a chlorine, bromine or iodine atom, or a group of -OSO2R<2>, in which R<2> is a methyl, tolyl or tri-fuloromethyl radical, with a substituted acetic acid derivative of the Formula R<1>CH2CO2Y wherein R<1> has the meaning as referred to; and Y is a hydrogen, sodium or potassium atom, or -NH4, an alkali metal salt or ammonium salt of the derivative, in the presence of ammonia. Among the 5-substituted-1-azabicycloÄ3.3.0Üoctanes, 5-cyanomethyl-1-azabicycloÄ3.3.0Üoctane can be converted into 5-(2-aminoethyl)-1-azabicycloÄ3.3.0Üoctane through a catalystic reduction which is carried out in atmospheric pressure, in alkali condition, and in the presence of Raney nickel.</p> |
