US2010105949A1PendingUtilityA1

Radiosynthesis of acid chlorides

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Assignee: HAMMERSMITH IMANET LTDPriority: Mar 20, 2004Filed: Jan 4, 2010Published: Apr 29, 2010
Est. expiryMar 20, 2024(expired)· nominal 20-yr term from priority
C07B 59/001
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Claims

Abstract

Radiolabelled acid chlorides may be synthesised by reacting a radiolabelled carboxylic acid with a solid-phase supported chlorinating agent.

Claims

exact text as granted — not AI-modified
1 - 24 . (canceled) 
   
   
       25 . A kit for carrying out a method for the preparation of a radiolabelled acid chloride compound of formula (I):
   R—COCl  (I)   wherein R is C 1 -C 20  alkyl, C 2 -C 20  alkenyl, C 3 -C 10  cycloalkyl, C 3 -C 10  heterocyclyl, C 4 -C 10  aryl or C 4 -C 10  heteroaryl, any of which may optionally be substituted with NO 2 , —O(C 1 -C 6  alkyl), C 3 -C 10  cycloalkyl or C 4 -C 10  aryl;   the method comprising reacting a radiolabelled carboxylic acid of formula (II):
   R—COOH  (II) 
   wherein R is as defined for formula (I);   with a solid-phase supported chlorinating agent in the presence of a base, the kit comprising:
 (i) a first cartridge containing a solid-phase supported chlorinating agent; and, 
 (ii) a vial containing a solution suitable for dissolving the radiolabelled carboxylic acid of formula (II), or components which can be reconstituted to form such a solution. 
   
   
   
       26 . A kit as claimed in  claim 25 , wherein the solid-phase supported chlorinating agent comprises a chlorinating agent connected by a linker to a solid support. 
   
   
       27 . A kit as claimed in  claim 25 , wherein the solution for dissolving the radiolabelled carboxylic acid of formula (II) also contains a base. 
   
   
       28 . A kit as claimed in any one of  claims 25  wherein the first cartridge contains a solid-phase supported base is immobilised on a solid support. 
   
   
       29 . A kit for the radiosynthesis of a radiolabelled product comprising a kit as claimed in  claim 25  and:
 (iii) a second cartridge containing a solid-phase supported non-radioactive precursor of the radiolabelled product.

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