Method for Producing Flutemetamol
AssigneesGe Healthcare Limited, Nihon Medi-Physics Co., Ltd.
InventorsYuki Okumura, Gota Tonoya, Tomoyuki Matsunami
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Abstract
Provided is a method for producing flutemetamol including the steps of: reacting a precursor compound represented by a predetermined general formula with a radioactive fluoride to obtain a 18F labeling compound represented by a predetermined general formula; allowing a strong base to act on the reaction mixture of the above step containing the precursor compound and the 18F labeling compound; after the above step, purifying the 18F labeling compound using a reverse phase solid phase extraction cartridge; and removing a protective group to obtain [18F]flutemetamol.
Claims20
A method for producing flutemetamol comprising the steps of:
- (a) reacting a compound represented by the following general formula (1) with a radioactive fluoride to obtain a compound represented by the following general formula (2);
- (b) allowing a strong base to act on the reaction mixture of the step (a) containing the compound represented by the general formula (1) and the compound represented by the general formula (2);
- (c) after the step (b), purifying the compound represented by the general formula (2) using a reverse phase solid phase extraction cartridge;
- and
- (d) removing a protective group to obtain [18F]flutemetamol.
- wherein R1 is a protective group of hydroxy, and C(O)R2 represents a protective group of amino.
- wherein R1 and R2 have the same meaning as in the compound represented by the general formula (1).
A method for producing flutemetamol comprising the steps of:
- (a) reacting a compound represented by the following general formula (1) with a radioactive fluoride to obtain a compound represented by the following general formula (2),
- wherein the group —OR1 is an ethoxymethoxy group or a methoxymethoxy group, and
- the group R2 is hydrogen or an alkyl having 1 to 10 carbon atoms;
- (b) allowing a strong base to act on the reaction mixture of the step (a) containing the compound represented by the general formula (1) and the compound represented by the general formula (2) to form a decomposition mixture;
- (c) purifying the decomposition mixture of step (b) to obtain the compound represented by the general formula (2) using a reverse phase solid phase extraction cartridge;
- (d) removing a protective group of the compound represented by the general formula (2) to obtain [18F]flutemetamol;
- (e) purifying the [18F]flutemetamol of step (d) using a reverse phase solid phase extraction cartridge to obtain [18F]flutemetamol purified after the first purification;
- and
- (f) further purifying the [18F]flutemetamol after the first purification of step (e) using a hydrophilic interaction solid phase extraction cartridge.
A method for producing flutemetamol comprising the steps of:
- (a) reacting a compound represented by the following general formula (1) with a radioactive fluoride to obtain a compound represented by the following general formula (2),
- wherein the group —OR1 is an ethoxymethoxy group or a methoxymethoxy group, and
- the group R2 is hydrogen or methyl;
- (b) allowing a strong base to act on the reaction mixture of the step (a) containing the compound represented by the general formula (1) and the compound represented by the general formula (2) to form a decomposition mixture;
- (c) purifying the decomposition mixture of step (b) to obtain the compound represented by the general formula (2) using a reverse phase solid phase extraction cartridge packed with triacontyl silylated silica gel;
- (d) removing a protective group of the compound represented by the general formula (2) to obtain [18F]flutemetamol;
- (e) purifying the [18F]flutemetamol of step (d) using a reverse phase solid phase extraction cartridge packed with triacontyl silylated silica gel to obtain [18F]flutemetamol purified after the first purification;
- and
- (f) further purifying the [18F]flutemetamol after the first purification of step (e) using a hydrophilic interaction solid phase extraction cartridge packed with aminopropylated silica gel.
Dependencies are inferred from the claim text.