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Process for production of precursor compound for radioactive halogen-labeled organic compound

A technology of organic compounds and precursor compounds, applied in the preparation of organic compounds, introduction of isotopes into organic compounds, organic chemical methods, etc., can solve problems such as stereo inversion

Active Publication Date: 2009-11-04
NIHON MEDI PHYSICS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Also, for [ 18 F]-FACBC, after introducing 18 Stereo inversion will occur in the step of F

Method used

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  • Process for production of precursor compound for radioactive halogen-labeled organic compound
  • Process for production of precursor compound for radioactive halogen-labeled organic compound
  • Process for production of precursor compound for radioactive halogen-labeled organic compound

Examples

Experimental program
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Effect test

Embodiment 1

[0060] Example 1: Synthesis of cis-1-(N-(tert-butoxycarbonyl)amino)-3-[((trifluoromethyl)sulfonyl)oxy]-cyclobutane-1-carboxylic acid ethyl ester

[0061] Hydrolysis of cis-hydantoin ( figure 1 ,step 1)

[0062] 250 mL of saturated barium hydroxide solution was added to 6.15 g (equivalent to 25 mmol) of 5-(3-benzyloxycyclobutane)hydantoin solution and heated to reflux in an oil bath at 114°C for 24 hours or longer time to obtain 1-amino-3-benzyloxycyclobutane-1-carboxylic acid. Then, TLC analysis was performed using two systems as developing solvents: chloroform / methanol = 5 / 1 (Rf value of cis-hydantoin = about 0.6) and chloroform / methanol = 95 / 1 (cis-hydantoin Rf value of urea = about 0.3), (by staining with UV and phosphomolybdic acid), the completion of the reaction was confirmed. Meanwhile, the cis / trans ratio of the hydantoin used in the reaction was about 65 / 35.

[0063] After the completion of the reaction was confirmed, the reaction solution was cooled to room tempe...

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Abstract

The present invention provides a process for producing a labeled precursor which is useful for the production of an amino acid compound labeled with a radioactive fluorine. In the reaction process for introducing a leaving group to a mixture of a syn-OH form and an anti-OH form of FACBC, a base is allowed to present in the reaction system to produce a syn-leaving group adduct which is unreactive with the base and is highly stable and an anti-leaving group adduct which can be react with the base to form a water-soluble compound. By employing a purification method utilizing the difference in solubility between these adducts, the syn-leaving group adduct can be separated selectively. The base may be a linear or branched primary to tertiary alkylamine having 1 to 10 carbon atoms, a nitrogenated heterocyclic compound having 2 to 20 carbon atoms or a nitrogenated hetero-aromatic cyclic compound having 2 to 20 carbon atoms.

Description

technical field [0001] The present invention relates to a process for the preparation of organic compounds which are suitable for the preparation of radiohalogen-labeled organic compounds which are active ingredients of formulations for positron emission tomography (PET). Background technique [0002] Nuclear medicine examinations can be performed by intravenously administering to humans a preparation containing a compound labeled with a specific radioisotope as an active ingredient (hereinafter referred to as "radiopharmaceutical") and detecting radiation emitted by the compound, and then imaging the information obtained from the radiation to diagnose. Nuclear medicine examinations are effective in the diagnosis of many diseases including heart diseases and cancers, and are characterized by not only high specificity and sensitivity for diseases but also the ability to provide information on damaged functions compared with other examination techniques. advantage. [0003] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C303/28C07C303/44C07C309/65A61K51/00C07B59/00G01T1/161G21G4/08
CPCG21H5/02C07B59/001C07C303/44A61K51/0406C07B2200/09C07C303/28C07C2101/04Y02P20/55C07C2601/04C07C309/73C07C309/65C07C309/66C07C213/08C07C219/24A61K51/00C07B59/00G01T1/161
Inventor 外山正人林明希男
Owner NIHON MEDI PHYSICS CO LTD