METHOD FOR THE PREPARATIONS OF DERIVATIVES OF 4A,5,9,10,11,12-HEXAHYDRO-6H-BENZOFURO [3A,3,2-EF] [2]BENZAZEPINE

摘要

The invention relates to a method enabling in particular thepreparation of galantamine with the formulathrough new bromo-N-demethylgalantamine with the formulaand new bromogalantamine with the formulaBy the method compound with formulaare recycled by oxidation to the compound having the formulawhich as reduced by L-Selektride diastereoselectively to the newbrom-N-dimethylgalantamine with the formulawithout the formation of proven quantities ofepibromo-N-demethylgalantamine. The new bromogalantanine withformula (5) is produced by methylation from which by brominesplitting, (±) galantamine is produced having formula (6). Theenantiomers in pure kind can be produced by the sedimentation as asalt of chiralic acid, in particular as tartarate. According tothe reaction scheme, high yields and pure products are produced inall stages so that the method can be applied on industrial scalesin its manufacture.