National Center for Geriatrics and Gerontology

Riken Corporation

Kinopharma, Inc.

Hiroko Koyama

Masaaki Suzuki

Hiroshi Ikenuma

Kengo Ito

Takamitsu Hosoya

Masatoshi Hagiwara

Takashi Kato

Hisashi Doi

Hiroshi Onogi

Toshiyuki Hiramatsu

Atsushi Natsume

The present invention provides a method for introducing substituents into the &#x3b1;-position and the &#x3b2;-position of an &#x3b1;,&#x3b2;-unsaturated ketone, which not only can be used for the synthesis of a prostaglandin by a three-component coupling process, but also enables synthesis of a prostaglandin in a high yield by one-pot operation without requiring the use of a large excess amount of any of the three components required for the synthesis or using a highly toxic heavy metal as a catalyst or a solvent that is highly toxic to living bodies, and a method for synthesizing a prostaglandin using the same technical means. The method for introducing substituents into an &#x3b1;,&#x3b2;-unsaturated ketone according to the present invention is a method for introducing substituents into the carbon at the &#x3b1;-position and the carbon at the &#x3b2;-position of an &#x3b1;,&#x3b2;-unsaturated ketone, including: a first step of mixing alkyllithium and trialkylalkenyl tin in which tin atom binds to the vinyl position of the alkenyl group; a second step of mixing the mixture of the first step and dialkylzinc; a third step of mixing the mixture of the second step and an &#x3b1;,&#x3b2;-unsaturated ketone; and a fourth step of mixing the mixture of the third step and a trifluoromethanesulfonate compound.

Method for introducing substituent into &#x3b1;,&#x3b2;-unsaturated ketone and method for synthesizing prostaglandin using the same

An object of the invention is to provide anC-labeled catechol derivative having sufficient radioactivity to obtain an imaging image by a PET apparatus, a PET probe of a phosphorylated tau aggregation inhibitor using the same, and a method for producing them. TheC-labeled catechol derivative of the present invention is represented by the following general formula (a) (wherein R is a substituent having an isopropylamino group, and the carbon at the 2-position of the isopropylamino group is labeled withC). 

11C-labeled catechol derivative, pet probe of phosphorylated tau aggregation inhibitor using the same, and production method of the same

An object of the invention is to provide aC-labeled O-benzylguanine capable of obtaining a PET image and a process for producing the same. TheC-labeled O-benzylguanine of the invention is represented by the following chemical formula (a). TheC-labeled O-benzylguanine is produced by: a coupling step of cross-coupling a methyl iodide labeled withC and the following organotin compound (b) (Rrepresents an alkyl group, and Rand Rrepresent a leaving group which can be eliminated with a base) in the presence of a palladium complex, a phosphine ligand, and cuprous halide in an aprotic lactam; and a desorption step of desorbing the leaving groups Rand Rof the coupling product obtained by the coupling step with a base. 

11C -labeled 06 -benzylguanine, pet probe capable of visualizing 06-methyl guanine methyl-transferase activity, and production method of the same

Provided is a method whereby a heteroaromatic ring aryl can be very rapidly methylated at a high yield. In an N-alkyl-2-pyrrolidinone, a heteroaromatic ring aryltrialkylstannan is cross-coupled with methyl iodide in the presence of a palladium complex, a phosphine ligand, a cuprous halide, a carbonic acid salt and/or an alkali metal fluoride to thereby rapidly methylate the heteroaromatic ring aryl. (Formula shows a case wherein the heteroaromatic ring aryl is a pyridyl group.) 

Method for rapidly methylating heteroaromatic arene and method for producing tracer for use in PET

Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.

Growing community of inventors

Gifu, Japan

Hiroko Koyama