METHOD OF PREPARING 4A,5,9,10,11,12-HEXAHYDRO-6H- BENZOFURO (3A,3,2-ef/2/BENZAZEPINE DERIVATIVES AND INTERMEDIATE COMPOUNDS Russian patent published in 2000 - IPC

Abstract RU 2146258 C1

FIELD: chemical industry. SUBSTANCE: described is method of preparing new 4a, 5,9,10,11,12-hexahydro-6H-benzofuro (3a,3,2-ef (2) benzazepine derivatives of general formula selected from group consisting of and or salts thereof wherein substituents are as defined in claim 1. Method comprises reacting (R2O)2C6H2(CHO)(X1) of formula III with compound of formula IV. The resulting condensation product is reduced, cyclized and is made to react with base and oxidizer. The resulting compound of general formula I wherein Y1 and Y2 are together=0 (ketone), reduced with L- selectride, K-selectride, KS-selectride and LS-selectride to compound of general formula I wherein Y1 is hydroxy, and racemic compound of general formula I wherein R4 is selected from group consisting of hydrogen, lower alkyl or aralkyl, is separated by crystallization by means of chiral acid to corresponding enantiomers. EFFECT: large amounts of the title compounds with higher yields both individual stages and in entire process. 28 cl, 40 ex

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RU 2 146 258 C1

Authors

Laslo Chollner

Jokhannes Frelikh

Ul'Rikh Jordis

Bernkhard Kjuenburg

Dates

2000-03-10Published

1995-10-23Filed