The separation of thevinone (2a) and beta-thevinone (2b), as well as t
hat of dihydrothevinone (3a) and beta-dihydrothevinone (3b) was accomp
lished. By the application of various procedures numerous new N-substi
tuted Diprenorphine analogues (8a-f) with 7R absolute configuration we
re synthesized. Detailed pharmacological investigation of the prepared
compounds may contribute to a better understanding of the structure-a
ctivity relationship of morphine alkaloids.