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. 1978 Apr;21(4):398-400.
doi: 10.1021/jm00202a018.

Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxone

I Iijima, J Minamikawa, A E Jacobson, A Brossi, K C Rice

Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxone

I Iijima et al. J Med Chem. 1978 Apr.

Abstract

(+)-Naloxone was prepared in 26% overall yield in eight steps from (+)-7-bromodihydrocodeinone dimethyl ketal by a synthesis which excluded enantiomeric contamination. (+)-Naloxone was examined in three assay systems and found to have no more than 1/1000(-1)/10 000th the activity of (-)-naloxone; it can, thus, serve to test the stereospecificity of the biochemical and pharmacological actions of (-)-naloxone.

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