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L. Czollner, J. Fröhlich, U. Jordis, B. Küenburg:
"Preparation of derivatives of 4a,5,9,10,11,12-hexahydro-6H-benzofuro[3a,3,2-ef][2]benzazepine";
Patent: U.S., Nr. 6043359; eingereicht: 18.04.1997, erteilt: 28.03.2000.

The invention relates to processes for the prepn. of 4a,5,9,10,11,12-hexahydro-6H-benzofuro[3a,3,2-ef][2]benzazepine, or derivs. thereof, e.g. of formula I [R1, R2, X1, X2, Y1, Y2 = H, halo, OH, alkoxy, alkyl, CHO, aryl, etc.; Y1Y2 = O]. Thus, 6-bromo-4-methoxy-3-hydroxybenzaldehyde and tyramine are condensed, then reduced and N-formylated. The product is then oxidatively cyclized to form the benzofuro[3a,3,2-ef][2]benzazepinone product, which is transformed into galanthamine. The racemic product is resolved by crystn. with (+)-di-p-toluoyl-D-tartaric acid.
AN 2000:205650