高須　清誠　　Dr. Kiyosei TAKASU
 

RESEARCH

業績要約

現在の研究テーマ（クリックすると要旨が出ます）

• 多置換環状物質を指向した合成法の開発
• 分子内ドミノ反応
• 分子間ドミノ反応
• 多成分反応
• 生理活性物質の合成と機能付加
• マラリア等熱帯病治療薬の開発

現在の興味の対象

• 多成分反応／カスケードプロセス
• プロセス合成
• 分子認識系を精密に利用した反応
• 特殊反応場
• 有機物質への機能付加
• ドラッグデリバリーシステム
• 大学発創薬　　　　　　　　　などなど

受賞

• ２０００年１２月
  日本薬学会東北支部奨励賞
  Encouraging Award in Pharmaceutical Society of Japan, Tohoku District
  「分子内連続反応の精密制御と生理活性物質合成への応用」

• ２００２年２月
  有機合成化学協会研究企画賞（藤沢薬品工業）
  Fujisawa Award in Synthetic Organic Chemistry, Japan
  「ブーメラン型マイケル−アルドール反応によるシクロブタン環構築法の開発と生理活性物質合成への応用」

• ２００３年１０月
  第３回天然物化学談話会奨励賞
  Young Scientistﾕs Research Award in Natural Product Chemistry
  「抗マラリア薬創製のための新戦略：生体膜内環境の特異を目指した分子設計」

• ２００５年２月
  有機合成化学奨励賞
  Incentive Award in Synthetic Organic Chemistry, Japan
  「求核付加を基盤とするドミノ反応の開発と物質合成への応用」

• ２００６年５月
  第５回インテリジェント・コスモス奨励賞
  Intelligent Cosmos Encouraging Award
  「マラリア等熱帯感染症の経口治療薬の開発」

博士学位論文

「cis-2,5-Diphenylpiperazine を有する化合物の構造と機能に関する研究」

発表論文

1. Convenient Synthesis of Substituted Piperidinones from a,b-unsaturatetd Amides: Formal Synthesis of Deplancheine, Tacamonine and Paroxetine,
   K. Takasu, N. Nishida, A. Tomimura, M. Ihara,
   J. Org. Chem., 2005, 70, 3957-3962.
2. Synthesis and Evaluation of β-Carbolinium Cations as New Antimalarial Agents Based on π-Delocalized　Lipophilic Cation (DLC) Hypothesis,
   K. Takasu, T. Shimogama, C. Saiin, K.-H. Sook, Y. Wataya, R. Brun, M. Ihara,
   Chem. Pharm. Bull., 2005, 53, 653-661.
3. A Practical Catalytic Method for Preparing Highly Substituted Cyclobutanes and Cyclobutenes,
   K. Inanaga, K. Takasu, M. Ihara,
   J. Am. Chem. Soc., 2005, 127, 3668-3669.
4. Synthesis of Medium-sized γ-Haloketones by Radical Mediated Ring-opening Reaction of Lewis Acid Catalyzed (2+2)-Cycloadducts,
   K. Takasu, S. Nagao, M. Ihara,
   Tetrahedron Lett., 2005, 46, 1005-1008.
5. Antileishmanial Activity of Rhodacyanine Dyes,
   K. Takasu, H. Terauchi, H. Inoue, M. Takahashi, S. Sekita, M. Ihara,
   Heterocycles, 2004, 64, 215-221.
6. 1-Aza-2-siloxybutadiene; Its Structure and Reactivity as a Piperidinone Synthon,
   K. Takasu, N. Nishida, M. Ihara,
   Synthesis, 2004, 2222-2225.
7. Palladium-Catalyzed Hydroamidation of Enones,
   K. Takasu, N. Nishida, M. Ihara,
   Synlett, 2004, 1844-1846.
8. 抗マラリア薬（大学での創薬研究）,
   井原正隆、高須清誠、寺内広毅
   Med. Chem. News, 2004, 14, (3) 14-17.
9. Rapid Assembly of Polycyclic Substances by a Multi-Component Cascade (4+2)-(2+2) Cycloadditions. The Total Synthesis of Proposed Structure of Paesslerin A,
   K. Inanaga, K. Takasu, M. Ihara,
   J. Am. Chem. Soc., 2004, 126, 1352-1353.
10. An Auxiliary Induced Asymmetric Synthesis of Functionalized Cyclobutanes by Means of Catalytic (2+2)-Cycloaddition Reaction,
    K. Takasu, S. Nagao, M. Ueno, M. Ihara,
    Tetrahedron, 2004, 60, 2071-2078.
11. π-Delocalized b-Carbolinium Cations As Potential Antimalarials,
    K. Takasu, T. Shimogama, C. Saiin, H.-S. Kim., Y. Wataya, M. Ihara,
    Bioorg. Med. Chem. Lett., 2004, 14, 1689-1692.
12. Catalytic (2+2)-Cycloaddition Reactions of Silyl Enol Ethers. A Convenient and Stereoselective Method for Cyclobutane Ring Formation,
    K. Takasu, M. Ueno, K. Inanaga, M. Ihara,
    J. Org. Chem., 2004, 69, 517-521.
13. A New Stereoselective Entry to Azaspirocyclic Nucleus of Halichlorine and Pinnaic Acide by Radical Translocation/Cyclization Reaction,
    K. Takasu, H. Ohsato, M. Ihara,
    Org. Lett., 2003, 5, 3017-3020.
14. A Direct Entry to Substituted Piperidones from α,β-Unsaturated Amides by Means of Aza Double Michael Addition,
    K. Takasu, N. Nishida, M. Ihara,
    Tetrahedron Lett., 2003, 44,7429-7432.
15. Parallel Synthesis of Antimalarial Rhodacyanine Dyes by the Combination of Three Components in One-Pot,
    K. Takasu, H. Terauchi, H. Inoue, H.-S. Kim, Y. Wataya, M. Ihara,
    J. Combi. Chem., 2003, 5, 211-214.
16. Asymmetric Intramolecular Aza-Michael Reaction Using Environmentally Friendly Organocatalysis,
    K. Takasu, S. Maiti, M. Ihara,
    Heterocycles, 2003, 51, 59-62.
17. Propylparaben: Physical characteristics,
    M. Rudyant, M. Ihara, K. Takasu, M. Yoshida, H. Poerwono, I. K. Indrayanto, H. G. Brittain,
    Anal. Prof. Drug Subst., Exc, Related Method., 2003, 30, 237-269.
18. Rhodacyanine Dyes as Antimalarials. 1. Antimalarial Activity and Toxicity of Rhodacyanine Dyes,
    K. Takasu, H. Inoue, H.-S. Kim, M. Suzuki, T. Shishido, M. Ihara,
    J. Med. Chem., 2002, 45, 995-998.
19. Novel Intramolecular (4+1) and (4+2) Annulation Reactions Employing Cascade Radical Cyclizations,
    K. Takasu, H. Ohsato, J. Kuroyanagi, M. Ihara,
    J. Org. Chem., 2002, 67, 6001-6007.
20. Unusual Regioselective Intramolecular Diels-Alder Reaction Forming Tricyclo[4.3.1.0^3,7]decane System,
    K. Takasu, S. Mizutani, M. Ihara,
    J. Org. Chem., 2002, 67, 2881-2884.
21. Cascade Radical Cyclization of Polyolefinic Vinyl Iodides: Comparison Between 5-exo and 6-endo Cyclization of Vinyl Radical,
    S. Maiti, K. Takasu, A. Katsumata, J. Kuroyanagi,
    ARKIVOC, 2002, 3 (vii), 197-211.
22. Asymmetric Synthesis of Tricyclic-cyclobutane by Means of Enantioselective Deprotonation and Intramolecular Michael-aldol Reaction,
    K. Takasu, K. Misawa,, M. Ihara,
    Tetrahedron Lett., 2001, 42, 8489-8491.
23. Facile and Stereoselective Access to Nonracemic Tricyclic Cyclobutanes by Asymmetric Intramolecular Michael-Aldol Reaction: Thermodynamic Equilibrium and Activation by Iodonium Ion,
    K. Takasu, M. Ueno, M. Ihara,
    J. Org. Chem., 2001, 66, 4667-4672.
24. Synthesis of a Novel Artemisinin Analogue Having Potent Antimalarial Activity,
    K. Takasu, R. Katagiri, Y. Tanaka, M. Toyota, H.-S. Kim, Y. Wataya, M. Ihara,
    Heterocycles, 2001, 54, 607-610.
25. Facile and Selective Formation of Linear-Triquinane Skeleton by Rationally Designed Round Trip Radical Reaction,
    K. Takasu, S. Maiti, A. Katsumata, M. Ihara,
    Tetrahedron Lett., 2001, 42, 2157-2160.
26. Conformation of 1,4-Dineopentyl-2,5-cis-diphenylpiperazine and Its Diammonium Salts: Remarkable Change in Conformation Depending upon the Counter Anion,
    K. Takasu, K. Tanaka, K. Fuji,
    Chem. Pharm. Bull., 2001, 49, 655-656.
27. ブーメラン型分子内連続反応の精密制御と生理活性物質合成への応用,
    高須清誠,
    薬学雑誌, 2001, 121, 887-898.
28. Novel Intramolecular (4+1) and (4+2) Annulations of Halopolyenes by Cascade Radical Reaction,
    K. Takasu, J. Kuroyanagi, M. Ihara,
    Org. Lett., 2000, 2, 3579-3581.
29. Auxiliary Induced Asymmetric Michael-Aldol Reaction under Kinetic and Thermodinamic Conditions,
    K. Takasu, M. Ueno, M. Ihara,
    Tetrahedron Lett., 2000, 41, 2145-2149.
30. Chiral Amine-Silyl Triflate Complex Mediated Asymmetric Intramolecular Michael-Aldol Reaction via a Novel Enantioselective Enol Silylation Process,
    K. Takasu, M. Misawa, M. Yamada, Y. Furuta, T. Taniguchi, M. Ihara,
    Chem. Commun., 2000, 1739-1740.
31. Palladium-Mediated Ring Closure Reactions. Facile Syntheses of Enantiopure Bicyclic and Tricyclic Alkenones,
    D. H. Hua, K. Takasu, X. Huang, G. S. Millward, Y. Chen, J. Fan,
    Tetrahedron, 2000, 56, 7389-7398.
32. Total Synthesis of (+/-)-Culmorin and (+/-)-Longiborneol: An Efficient Construction of Tricyco[6.3.0.0^3,8]undecan-10-one by Intramolecular Double Michael Addition,
    K. Takasu, S. Mizutani, M. Noguchi, K. Makita, M. Ihara,
    J. Org. Chem., 2000, 65, 4112-4119.
33. Conformational Difference between Mono- and Diprotonated cis-2,5-Diphenylpiperazinium Salts in the Solid State,
    K. Takasu, H. Miyamoto, K. Tanaka, T. Taga, M. Bando, K. Fuji,
    Chem. Pharm. Bull., 2000, 48, 2014-2016.
34. 6-endo,6-endo,6-exo Cascade Cyclization Starting from Vinyl Radical; Construction of Dodecahydrophenanthrene System,
    K. Takasu, J. Kuroyanagi, A. Katsumata, M. Ihara,
    Tetrahedron Lett., 1999, 40, 6277-6280.
35. Stereocontrolled Total Synthesis of (+/-)-Culmorin via the Intramolecular Double Michael Addition,
    K. Takasu, S. Mizutani, M. Noguchi, K. Makita, M. Ihara,
    Org. Lett., 1999, 1, 391-394.
36. 5-exo,5-exo Cascade Cyclizations of Halo-olefins by Environmentally Friendly Reaction Using Indirect Electrolysis,
    A. Katsumata, K. Takasu, M. Ihara,
    Heterocycles, 1999, 51, 733-736.
37. Facile Construction of the Tricyclo[5.2.1.0^1,5]decane Ring System by Intramolecular Double Michael Reaction: Highly Stereocontrolled Total Synthesis of (+/-)-8,14-Cedranediol and (+/-)-8,14-Cedranoxide,
    M. Ihara, K. Makita, K. Takasu,
    J. Org. Chem., 1999, 64, 1259-1264.
38. Chiral Sulfur-Containing 1,2-Disubstituted Ferrocenes,
    N. M. Lagneau, Y. Chen, P. M. Robben, H.-S. Sin, K. Takasu, J.-S. Chen, P. D. Robinson, D. H. Hua,
    Tetrahedron, 1998, 54, 7301-7334.
39. Nonenzymatic Kinetic resolution of Racemic Alcohols through an "Induced Fit" Process,
    T. Kawabata, M. Nagato, K. Takasu, K. Fuji,
    J. Am. Chem. Soc., 1997, 119, 3169-3170.
40. Polyaza Macrocycles Containing the Piperazine Ring as a Semi-Flexible Moiety,
    K. Fuji, K. Takasu, H. Miyamoto, K. Tanaka, Y. Miwa, T. Taga,
    Tetrahedron Lett., 1996, 37, 7111-7114.
41. Facile Synthesis of Optically Active cis-2,5-Diphenyl-1,4-Diazabicyclo[2.2.2]octane,
    K. Fuji, K. Tanaka, K. Takasu,
    Tetrahedron: Asymmetry, 1996, 7, 1749-1751.
42. Chiral Recognition of Amino Acid Derivatives by 1,1'-Binaphthalene-8,8'-diol,
    T. Kawabata, A. Kuroda, E. Nakata, K. Takasu, K. Fuji,
    Tetrahedron Lett., 1996, 37, 4153-4156.

特許

PROFILE

• 誕生日　　1970.12.12
• 出身地　　京都
• 座右の銘　どんなに道が険しくても、笑いながら歩け！
• 趣味　　　プロレス、笑うこと、芸能、ウクレレ
• 特技　　　科学、フェンシング、妄想
• 夢　　　　細胞を作る！
• ひとこと　どんなことでもやれるだけで儲けもん