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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-L-dopa

A protected 6-trimethylstannyl dopa derivative has been synthesized for the as a precursor for the preparation of 6-[.sup.18 F]fluoro-L-dopa. The tin derivative readily reacts with electrophilic radiofluorinating agents such as [.sup.18 F]F.sub.2, [.sup.18 F]OF.sub.2 and [.sup.18 F]AcOF. The [.sup.18 F]fluoro intermediate was easily hydrolyzed with HBr and the product 6-[.sup.18 F]fluoro-L-dopa was isolated after HPLC purification in a maximum radiochemical yield of 23%, ready for human use.
Inventors:
 [1];  [2];  [3];  [4]
  1. (1613 Barry Ave. - Apt. #9, Los Angeles, CA 90025)
  2. (5920 Grey Rock Rd., Agoura Hills, CA 91301)
  3. (1661 Selby Ave. - Apt. 5A, Los Angeles, CA 90024)
  4. (3230 Overland Ave. - Apt. 121, Los Angeles, CA 90034)
Issue Date:
OSTI Identifier:
869766
Assignee:
Satyamurthy, Nagichettiar (1613 Barry Ave. - Apt. #9, Los Angeles, CA 90025);Barrio, Jorge R. (5920 Grey Rock Rd., Agoura Hills, CA 91301);Bishop, Allyson J. (1661 Selby Ave. - Apt. 5A, Los Angeles, CA 90024);Namavari, Mohammad (3230 Overland Ave. - Apt. 121, Los Angeles, CA 90034) OAK
Patent Number(s):
US 5393908
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-l-dopa; protected; 6-trimethylstannyl; dopa; derivative; synthesized; precursor; preparation; readily; reacts; electrophilic; radiofluorinating; agents; acof; fluoro; intermediate; easily; hydrolyzed; hbr; product; isolated; hplc; purification; maximum; radiochemical; yield; 23; human; regioselective radiofluorodestannylation; fluorinating agent; ethyl ester; -l-phenylalanine ethyl; /999/

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