The Asan Foundation

Futurechem Co., Ltd

Industry-university Cooperation Foundation Sogang University

Jin-sook Ryu

Dae Yoon Chi

Seung Jun Oh

Jae-seung Kim

Dae Hyuk Moon

Seung-jun Oh

Dae-hyuk Moon

Dong Wook Kim

Jong-Jin Lee

Jae Seung Kim

Chansoo Park

Dae-Yoon Chi

Byoung Se Lee

So Young Chu

Byoung-Se Lee

Yu Jin Bae

So-Young Chu

Uthaiwan Sirion

Yoo Jin Lim

Heejun Kim

Sang-ju Lee

Sirion Uthaiwan

Yu-Jin Bae

Youjung Jung

A method for preparing a radiopharmaceutical and, specifically, a method for preparing an organic fluoride-aliphatic compound usable as a radiopharmaceutical, a method for purifying the prepared organic fluoride-aliphatic compound, and a method for preparing a radiopharmaceutical by using a cassette comprising a backdraft preventing reaction container. A method for preparing an organic fluorinated aliphatic compound includes allowing a fluorine salt to react with a leaving group-containing aliphatic compound by using a multifunctional solvent represented by the following Chemical Formula 1 to obtain an aliphatic compound labeled with [F] fluoride substituting for the leaving group. The organic fluoride-aliphatic compound can be prepared and purified through even a simple process at high yield, high efficiency, and high purity, and the radiopharmaceutical can be safely prepared without damage to a synthetic apparatus.

Method for preparing organic fluoride-aliphatic compound and method for purifying organic fluoride-aliphatic compound

The present invention relates to (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or to the pharmaceutically acceptable salt thereof, to a method for preparing same, and to a pharmaceutical composition containing same as active ingredients for the diagnosis or treatment of neurodegenerative brain diseases. The aryl derivatives of the present invention are (3-fluoro-2-hydroxy)propyl-functionalized to increase the polarity thereof, and therefore the drugs containing the aryl derivatives can easily permeate into the cerebrovascular membrane, thus increasing the effectiveness of the drugs. As the aryl derivatives of the present invention strongly bind to &#x3b2;-amyloid, the aryl derivatives, when labeled with radioisotope, can be used as a diagnostic agent for non-invasively diagnosing early Alzheimer's disease. Further, the aryl derivatives of the present invention bind to low molecular &#x3b2;-amyloid peptide conjugates to inhibit the generation of malignant high molecular &#x3b2;-amyloid plaque, and thus can be effectively used as a therapeutic agent for neurodegenerative brain diseases such as Alzheimer's disease.

(3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or pharmaceutically acceptable salts thereof, method for preparing same, and pharmaceutical composition containing same as active ingredient for the diagnosis or treatment of neurodegenerative brain diseases

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

Jin-sook Ryu