Back to results
US 10,059,661 B1Granted
Method of fabricating [F-18]FEONM precursor
AssigneeINTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, Executive Yuan, R.O.C.
InventorsShu-Hung Lin, Sheng-Po Huang, Show-Wen Liu, Cheng-Fang Hsu, Jenn-Tzong Chen, Shiou-Shiow Farn, Wuu-Jyh Lin, Chyng-Yann Shiue
Life of this patent
Estimating the term…
Abstract
A [F-18]FEONM precursor is synthesized. 2-bromoethanol is added to further connect an atom of oxygen at an N terminal of the precursor. Four atoms of carbon can be further connected. Thus, better fat-solubility is obtained along with the increase in carbon. Positioning in brain imaging becomes better.
Claims6
A method of fabricating a [F-18]FEONM precursor, comprising steps of:
- (a) adding a first compound of 2-acetyl-6-methoxynaphthalene as a starting material in a concentrated hydrochloric acid (HCl) solution to be mixed at an equivalence ratio of 1±20 percents (%):60±20% of said first compound to HCl;
- heating to reflux overnight to turn solution color from yellow to black;
- and obtaining a second compound after purification;
- (b) under an argon condition, adding said second compound, deionized pure water, 2-methylaminoethanol and sodium metabisulfite (Na2O5S2) to be mixed at an equivalence ratio of 1±20%:0.08±20% of said second compound to 2-methylaminoethanol;
- heating to 100 celsius degrees (° C.)±20% with stirring to reflux for 94±20% hours to turn solution color from black to yellow;
- monitoring reaction through thin layer chromatography (TLC) with a ratio of 1:1 of ethyl acetate (EtOAc) to n-hexane;
- and obtaining a third compound after purification;
- (c) under an argon condition, adding said third compound and malononitrile (CH2(CN)2);
- implanting anhydrous pyridine to be mixed at an equivalence ratio of 1±20%:4±20% of said third compound to CH2(CN)2;
- heating to 70° C.±20% with stirring to reflux for 4±20% hours;
- monitoring reaction through TLC with a ratio of EtOAc:n-hexane=1:1;
- and obtaining a fourth compound after purification;
- (d) under an argon condition, adding said fourth compound, potassium carbonate (K2CO3), anhydrous dimethylformamide (DMF) and 2-bromoethanol to be mixed at an equivalence ratio of 1±20%:3±20%:3±20% of said fourth compound to K2CO3 and 2-bromoethanol;
- heating to 90° C.±20% with stirring to reflux overnight;
- monitoring reaction through TLC with a ratio of EtOAc:n-hexane=1:1;
- and obtaining a fifth compound after purification;
- (e) under an argon condition, adding said fifth compound, p-toluenesulfonyl chloride (TsCl), anhydrous dichloromethane (CH2Cl2) and anhydrous pyridine to be mixed at an equivalence ratio of 1±20%:4±20% of said fifth compound to TsCl;
- stirring under a room temperature for 5±20% hours;
- monitoring reaction through TLC with a ratio of EtOAc:n-hexane=1:1;
- and obtaining a precursor of [F-18]FEONM,
- wherein said precursor of [F-18]FEONM has a chemical structural formula as follows:
18 more elements
Dependencies are inferred from the claim text.