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クリックケミストリー 創薬研究のための新しいツール

創薬研究のための新しいツール クリックケミストリーのための有機合成用試薬

クリックケミストリーは、2001年にスクリプト研究所のシャープレス教授(2001年ノーベル化学賞受賞)が 提唱した比較的簡単な構造を持つパーツ同士を高い反応性・選択制を持つ炭素-ヘテロ原子結合反応によって結びつけることにより、 新たな機能性分子を創出させる可能性を持たせた手法です。


  • 簡単な構造を持つパーツ同士の組み合>わせによる反応
  • 広い適用範囲
  • 高収率
  • 有害な副産物不産出
  • 出発原料が容易に入手可能

1961年にR.ヒュスゲン(R. Huisgen)によって開発されたアジドとアルキンから1,2,3-トリアゾールを合成する1,3-双極子付加環化反応(1,3-dipolar cycloaddition of alkynes and azides)はクリックケミストリーの代表的な例としてあげることができます。

クリックケミストリー反応で要求される特色の一つに「原料の入手が容易であること」があげられますが、 AMT社はこの目的を達成するためにクリックケミストリー反応用として利用できる様々な官能性アルキンやアジドを有する化合物用意しました。


(1) Click Chemistry: Diverse Chemical Function from a Few Good Reactions,
H.C. Kolb, M.G. Finn and K.B. Sharpless. Angew. Chem. Int. Ed., 2001, 40, 2004
(2) Click Chemistry Reactions in Medicinal Chemistry: Applications of 1,3-Dipolar Cycloadditions between Azides and Alkynes
G. C. Tron, T. Pirali, R. A. Billington, P. L. Canonico and A. A. Genazzani. Medicinal Chemistry Reviews, 2008, 28, 278
(3) A Modular Approach to Catalytic Synthesis Using a Dual-functional Linker for Click and Suzuki Coupling Reactions
J. R. White, G. J. Price, S. Schiffers, P. R. Raithby, P. K. Plucinski nd C. G. Frost. Tetrahedron Letters, 2010, 51, 3913
(4) Highly Sensitive Detection of Saccarides Under Physiological Conditions with Click Synthesized Boronic Acid-ologomer
K. Mulla, P. Dongare, Z. Ningzhang, G. Chen, D. Thompson and Y. Zhao. Organic & Biomolecular Chemistry, 2011 , 9, 1332
(5) Synthesis of Functionalized Organotrifluoroborates via the 1,3-Dipolar Cycloaddtion of Azides
G. A. Molander and J. Ham. Organic Letters, 2006, 8, 2767

Click Chemistry & Microwaves References

Microwave-mediated click-chemistry’ synthesis of glyco-porphyrin derivatives and in vitro photo-cytotoxicity for application in photodynamic therapy
Garcia, Guillaume; Naud-Martin, Delphine; Carrez, Daniele; Croisy, Alain; Maillard, Philippe
Tetrahedron (2011), 67(26), 4924-4932

Microwave assisted click chemistry on a conductive polymer film
Daugaard, Anders E.; Hansen, Thomas S.; Larsen, Niels B.; Hvilsted, Soren
Synthetic Metals (2011), 161(9-10), 812-816

Click chemistry under microwave or ultrasound irradiation
Barge, Alessandro; Tagliapietra, Silvia; Binello, Arianna; Cravotto, Giancarlo
Current Organic Chemistry (2011), 15(2), 189-203

Microwave irradiated click reactions on silicon surfaces via derivatization of covalently grafted poly(PEGMA) brushes
Liu, Xiang; Zheng, Hong-Ning; Ma, Yin-Zhou; Yan, Qing; Xiao, Shou-Jun
Journal of Colloid and Interface Science (2011), 358(1), 116-122

Click-Reagent Version of Sonogashira Coupling Protocol to Conjugated Fluorescent Alkynes with No or Reduced Homocoupling
Bag, Subhendu Sekhar; Kundu, Rajen; Das, Manas
Journal of Organic Chemistry (2011), 76(7), 2332-2337.

Versatile Site-Specific Conjugation of Small Molecules to siRNA Using Click Chemistry
Yamada, Takeshi; Peng, Chang Geng; Matsuda, Shigeo; Addepalli, Haripriya; Jayaprakash, K. Narayanannair; Alam, Md. Rowshon; Mills, Kathy; Maier, Martin A.; Charisse, Klaus; Sekine, Mitsuo; et al
Journal of Organic Chemistry (2011), 76(5), 1198-1211

Microwave-accelerated click chemistry: expeditious synthesis of novel triazole-linked salicylic β-D-O-glycosides with PTP1B inhibitory activity
Yang, Jin-Wei; Li, Cui; He, Xiao-Peng; Zhao, Hong; Gao, Li-Xin; Zhang, Wei; Shi, Xiao-Xin; Tang, Yun; Li, Jia; Chen, Guo-Rong
Bulletin of the Korean Chemical Society (2010), 31(11), 3359-3365

Expeditious preparation of triazole-linked glycolipids via microwave accelerated click chemistry and their electrochemical and biological assessments
Song, Shao-Xing; Zhang, Hai-Lin; Kim, Chol-Guk; Sheng, Li; He, Xiao-Peng; Long, Yi-Tao; Li, Jia; Chen, Guo-Rong
Tetrahedron (2010), 66(52), 9974-9980

A Straightforward Preparation of Aminoglycoside-Dinucleotide and -diPNA Conjugates via Click Ligation Assisted by Microwaves
Alguacil, Javier; Defaus, Sira; Claudio, Ana; Trapote, Alejandro; Masides, Marta; Robles, Jordi
European Journal of Organic Chemistry (2010), (16), 3102-3109

Click chemistry under non-classical reaction conditions
Kappe, C. Oliver; Van der Eycken, Erik
Chemical Society Reviews (2010), 39(4), 1280-1290

Efficient Synthesis of Glycoporphyrins by Microwave-Mediated "Click" Reactions
Locos, Oliver B.; Heindl, Claudia C.; Corral, Ariadna; Senge, Mathias O.; Scanlan, Eoin M.
European Journal of Organic Chemistry (2010), (6), 1026-1028

Microwave-assisted click chemistry: Synthesis of mono and bis-1,2,3-triazole acyclonucleoside analogues of Acyclovir via copper(I)-catalyzed cycloaddition
Krim, J.; Sillahi, B.; Taourirte, M.; Rakib, E. M.; Engels, J. W.
ARKIVOC (Gainesville, FL, United States) (2009), (13), 142-152

Microwave-assisted click polymerization for the synthesis of Aβ(16-22) cyclic oligomers and their self-assembly into polymorphous aggregates
Elgersma, Ronald C.; van Dijk, Maarten; Dechesne, Annemarie C.; van Nostrum, Cornelus F.; Hennink, Wim E.; Rijkers, Dirk T. S.; Liskamp, Rob M. J.
Organic & Biomolecular Chemistry (2009), 7(21), 4517-4525

icrowave-assisted benzyne-click chemistry: preparation of 1H-benzo[d][1,2,3]triazoles
Ankati, Haribabu; Biehl, Ed
Tetrahedron Letters (2009), 50(32), 4677-4682

Synthesis and Characterization of Biodegradable Peptide-Based Polymers Prepared by Microwave-Assisted Click Chemistry
van Dijk, Maarten; Nollet, Maria L.; Weijers, Pascal; Dechesne, Annemarie C.; van Nostrum, Cornelus F. n; Hennink, Wim E.; Rijkers, Dirk T. S.; Liskamp, Rob M. J.
Biomacromolecules (2008), 9(10), 2834-2843

Microwave enhancement of a "one-pot" tandem azidation-"click" cycloaddition of anilines
Moorhouse, Adam D. and Moses, John. E.
Synlett (2008), (14), 2089-2092





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