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Title: Synthesis of N-formyl-3,4-di-t-butoxycarbonyloxy-6-(trimethylstannyl)-L-phenylalanine ethyl ester and its regioselective radiofluorodestannylation to 6- .sup.18 F!fluoro-1-dopa

A process for forming a 6-fluoro derivative of compounds in the L-Dopa family comprising the steps of protecting the groups attached to the benzene ring in the compound followed by serially reacting the protected compound with (a) iodine and silver trifluoroacetic acid; (b) Bb.sub.3 ; (c) dit-butyldicarbonate; (d) hexamethyltin; (e) a fluoro compound; (f) hydrobromic acid; and (g) raising the pH to .ltoreq.7.
Inventors:
 [1];  [2];  [3];  [1];  [4]
  1. (Los Angeles, CA)
  2. (Agoura Hills, CA)
  3. (Wahnemuhle, DE)
  4. (Shreveport, LA)
Issue Date:
OSTI Identifier:
870385
Assignee:
Regents of University of California (Oakland, CA) OAK
Patent Number(s):
US 5510522
Contract Number:
FC03-87ER60615
Research Org:
University of California
Country of Publication:
United States
Language:
English
Subject:
synthesis; n-formyl-3; 4-di-t-butoxycarbonyloxy-6-; trimethylstannyl; -l-phenylalanine; ethyl; ester; regioselective; radiofluorodestannylation; 6-; 18; fluoro-1-dopa; process; forming; 6-fluoro; derivative; compounds; l-dopa; family; comprising; steps; protecting; attached; benzene; compound; followed; serially; reacting; protected; iodine; silver; trifluoroacetic; acid; bb; dit-butyldicarbonate; hexamethyltin; fluoro; hydrobromic; raising; ph; ltoreq; acetic acid; regioselective radiofluorodestannylation; ethyl ester; -l-phenylalanine ethyl; /999/

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