The Asan Foundation

Industry-university Cooperation Foundation Sogang University

Futurechem Co., Ltd

Dae Hyuk Moon

Seung Jun Oh

Dong Wook Kim

Jong Jin Lee

Jae Seung Kim

Dae Yoon Chi

Jin-sook Ryu

Byoung Se Lee

So Young Chu

Sang Ju Lee

Yu Jin Bae

Heejun Kim

Yoo Jin Lim

Uthaiwan Sirion

Youjung Jung

Jin-Sook Ryu

Seung Jun 205-501 Yuwon 2Ch Ap Oh

The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [F]fluoride in a method for preparing an organic [F]fluoro compound by reacting an alkyl halide or an alkyl sulfonate with a [F]fluoride, wherein a [F]fluoride supported on a quaternary alkyl ammonium polymer support is eluted using a solution containing a metal salt or a quaternary ammonium salt with an adjusted pH, and a base is not additionally used. The present invention enables a labeling reaction without an additional base after precisely reflecting the concentration of a base absolutely necessary for the nucleophilic substitution of a [F]fluoride or eluting a [F]fluoride using a [F]fluoride eluent with an adjusted pH, thereby stably obtaining a [F]fluoride-labelled compound in a high yield, and is thus useful for production of fluorine-18-labelled radioactive medical supplies.

Method for preparing fluorine-18 eluent with adjusted PH, and method for labelling fluorine-18 using same

2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for &#x3b2;-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes: wherein R-R, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight &#x3b2;-amyloid peptide binding compound, generation of malignant high-molecular weight &#x3b2;-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.

2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, preparation method thereof, and pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as active ingredient

The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of primary or secondary organofluoro compound by reacting fluorine salt containing radioactive isotope fluorine-18 with primary or secondary alkyl halide or primary or secondary alkyl sulfonate in the presence of alcohol of Chemical Formula 1 as a solvent to obtain high yield of organofluoro compound. Synthesis reaction according to the present invention may be carried out under mild condition to give high yield of the organofluoro compounds and the reaction time is decreased, and thereby is suitable for the mass production of the organofluoro compounds.

Method for preparation of F-18 containing organofluoro compounds in alcohol solvents

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Seoul, South Korea

Dae Hyuk Moon