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 Title: |
US5510522:
Synthesis of N-formyl-3,4-di-t-butoxycarbonyloxy-6-(trimethylstannyl)-L-phenylalanine ethyl ester and its regioselective radiofluorodestannylation to 6-[18 F]fluoro-1-dopa
[ Derwent Title ]
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| Country: |
US United States of America
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| Inventor: |
Satyamurthy, Nagichettiar; Los Angeles, CA
Barrio, Jorge R.; Agoura Hills, CA
Bishop, Allyson J.; Wahnemuhle, Germany
Namavari, Mohammad; Los Angeles, CA
Bida, Gerald T.; Shreveport, LA
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| Assignee: |
Regents of the University of California, Oakland, CA
other patents from UNIVERSITY OF CALIFORNIA, THE REGENTS OF (599425) (approx. 4,840)
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| Published / Filed: |
1996-04-23
/ 1995-02-22
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| Application Number: |
US1995000393428
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| IPC Code: |
Advanced:
C07B 59/00;
C07C 215/52;
C07C 229/36;
Core:
C07C 215/00;
C07C 229/00;
more...
IPC-7:
C07C 229/00;
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| ECLA Code: |
C07B59/00C; C07C215/52; C07C229/36;
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| U.S. Class: |
Current:
562/446;
Original:
562/446;
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| Field of Search: |
562/446
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| Government Interest: |
This invention was made in part with government support from a Department of Energy Grant DE-FC0387-ER60615, NIH Grant PO1-NS-15654 and NIMH Grant RO1-MH-37916.
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| Priority Number: |
| 1995-02-22 |
US1995000393428 |
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| Abstract: |
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) Bb3 ; (c) dit-butyldicarbonate; (d) hexamethyltin; (e) a fluoro compound; (f) hydrobromic acid; and (g) raising the pH to <=7.
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| Primary / Asst. Examiners: |
Nazario-Gonzales, Porfiro;
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| INPADOC Legal Status: |
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| Parent Case: |
This is a Continuation-In-Part of U.S. application Ser. No. 07/903,915 filed on Jun. 25, 1995, now U.S. Pat. No. 5,393,908.
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| Family: |
None
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First Claim:
Show all 3 claims |
What is claimed is:
1. The process of forming 6-fluoro derivatives of a benzene containing chemical compound selected from the group consisting of L-DOPA and chemicals in the L-DOPA family comprising the steps of:
- (a) in the presence of acetic anhydride, reacting the chemical compound containing a benzene ring with a second chemical compound capable of protecting a chemical moiety on the first benzene carbon,
- (b) reacting the product of step (a) with iodine and silver trifluoroacetate,
- (c) reacting the product of step (b) with BBr3,
- (d) reacting the product of step (c) with di t-butyl dicarbonate,
- (e) reacting the product of step (d) with hexamethyliditin;
- (f) bubbling an unlabelled or radiolabeled fluorine compound selected from the group consisting of [18 F]CH3 COOF, [18 F]F2, and [18 F]OF2 and combinations thereof through the product of step (e);
- (g) treating the product of step (f) above with hydrobromic acid;
- (h) raising the pH of the product of step (g) above to a value <=7 by the addition of NaOH.
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| Background / Summary: |
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| Drawing Descriptions: |
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| Description: |
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| Forward References: |
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