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

✍ Scribed by Stephen P. O'Connor; Robert L. Ellsworth; Gregory Gatto; Merck Sharp; Dohme


Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
258 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

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‐^14^C]‐propanamine (Z)‐2‐butenedioate(1:1) (11, [^14^C]L‐637,510), a potential muscle relaxant product for which ^14^C‐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 [^14^C]cyanide with an overall radiochemical yield of 4.8%.


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