Synthesis of the muscle relaxant [14C]L-637,510

The synthesis of (E)‐3‐(9‐chloro‐5,6‐dihydro‐1 1 H‐pyrrolo(2,1‐b)(3)‐benzazepin‐11‐ylidene)‐N, N‐dimethyl‐1‐[3‐14C]‐propanamine (Z)‐2‐butenedioate(1:1) (11, [14C]L‐637,510), a potential muscle relaxant product for which 14C‐labeling was required for metabolism studies, is described. Introduction of...

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Veröffentlicht in:Journal of labelled compounds & radiopharmaceuticals 1991-07, Vol.29 (7), p.791-796
Hauptverfasser: O'Connor, Stephen P., Ellsworth, Robert L., Gatto, Gregory, Sharp, Merck, Dohme
Format: Artikel
Sprache:eng
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Zusammenfassung:The synthesis of (E)‐3‐(9‐chloro‐5,6‐dihydro‐1 1 H‐pyrrolo(2,1‐b)(3)‐benzazepin‐11‐ylidene)‐N, N‐dimethyl‐1‐[3‐14C]‐propanamine (Z)‐2‐butenedioate(1:1) (11, [14C]L‐637,510), a potential muscle relaxant product for which 14C‐labeling was required for metabolism studies, is described. Introduction of the label in the 3‐position of the propanamine side chain was accomplished in eight steps from sodium [14C]cyanide with an overall radiochemical yield of 4.8%.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.2580290709