Method for producing [18F]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 [18F]flutemetamol comprising the steps of:
- (a) reacting a compound of formula (1) with a reactive fluoride
- wherein
- —OR1 is selected from hydroxyl or an alkoxymethoxy group having 1 to 6 carbon atoms, and
- R2 is selected from hydrogen, alkyls having 1 to 10 carbon atoms, haloalkyls having 1 to 10 carbon atoms, aryls having 6 to 14 carbon atoms, arylalkyls having 6 to 14 carbon atoms, or —(CH2CH2O)p—CH3 wherein p is an integer of 1 to 10;
- wherein the reaction of step (a) results in a reaction mixture of the compound of formula (1) and a compound of formula (2):
- (b) exposing the reaction mixture of step (a) to a strong base, the reaction mixture of step (a) comprising the compound of formula (1) and the compound of formula (2);
- (c) after the step (b), purifying the compound of formula (2) using a reverse phase solid phase extraction cartridge;
- and
- (d) removing a protective groups to obtain [18F]flutemetamol.
A method for producing [18F]flutemetamol comprising the steps of:
- (a) reacting a compound of formula (1) with a radioactive fluoride to obtain a compound of 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 of formula (1) and the compound of formula (2) to form a decomposition mixture;
- (c) purifying the decomposition mixture of step (b) to obtain the compound of formula (2) using a reverse phase solid phase extraction cartridge;
- (d) removing a protective group of the compound of 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 [18F]flutemetamol comprising the steps of:
- (a) reacting a compound of formula (1) with a radioactive fluoride to obtain a compound of 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 of formula (1) and the compound of formula (2) to form a decomposition mixture;
- (c) purifying the decomposition mixture of step (b) to obtain the compound of formula (2) using a reverse phase solid phase extraction cartridge packed with triacontyl silylated silica gel;
- (d) removing a protective group of the compound of 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.