Synthesis 2014; 46(02): 195-202
DOI: 10.1055/s-0033-1338563
paper
© Georg Thieme Verlag Stuttgart · New York

Catalytic C–H Activation of Arylacetylenes: A Fast Assembly of 3-(Arylethynyl)-3-hydroxyindolin-2-ones Using CuI/DBU

Mangilal Chouhan
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, Mohali, Punjab 160062, India   eMail: vn74nr@yahoo.com
,
Kishna Ram Senwar
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, Mohali, Punjab 160062, India   eMail: vn74nr@yahoo.com
,
Kapil Kumar
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, Mohali, Punjab 160062, India   eMail: vn74nr@yahoo.com
,
Ratnesh Sharma
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, Mohali, Punjab 160062, India   eMail: vn74nr@yahoo.com
,
Vipin A. Nair*
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, Mohali, Punjab 160062, India   eMail: vn74nr@yahoo.com
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Publikationsverlauf

Received: 27. August 2013

Accepted after revision: 29. Oktober 2013

Publikationsdatum:
28. November 2013 (online)


Abstract

A highly efficient and atom-economic methodology has been developed for the synthesis of 3-(arylethynyl)-3-hydroxyindolin-2-ones from isatins by C–H activation of arylacetylenes using a catalytic quantity of copper(I) iodide (5 mol%) and DBU (20 mol%) at 25 °C, affording the products in excellent yields in very short reaction time (5 min).

Supporting Information

 
  • References

    • 1a Frantz DE, Fässler R, Tomooka CS, Carreira EM. Acc. Chem. Res. 2000; 33: 373
    • 1b Li CJ. Acc. Chem. Res. 2010; 43: 581
    • 1c Fujimori S, Knöpfel TF, Zarotti P, Ichikawa T, Boyall D, Carreira EM. Bull. Chem. Soc. Jpn. 2007; 80: 1635
    • 1d Trost BM, Weiss AH. Adv. Synth. Catal. 2009; 351: 963
  • 2 Kumagai N, Matsunaga S, Shibasaki M. J. Am. Chem. Soc. 2004; 126: 13632 ; and references cited therein
    • 3a Cozzi PG, Hilgraf R, Zimmermann N. Eur. J. Org. Chem. 2004; 4095
    • 3b Modern Acetylene Chemistry . Diederich F, Stang PJ. VCH; Weinheim: 1995
    • 4a Marshall JA, Bourbeau MP. Org. Lett. 2003; 5: 3197
    • 4b Siemsen P, Livingston RC, Diederich F. Angew. Chem. Int. Ed. 2000; 39: 2632
    • 5a Sarciron ME, Audin P, Delabre I, Gabrion C, Petavy AF, Paris J. J. Pharm. Sci. 1993; 82: 605
    • 5b Brummond KM, Osbourn JM. Beilstein J. Org. Chem. 2010; 6: 33
    • 5c Dong Y.-W, Wang G.-W, Wang L. Tetrahedron 2008; 64: 10148
    • 6a Makaiyama T, Suzuki K, Sato T. Chem. Lett. 1979; 447
    • 6b Tombo GM. R, Didier E, Loubinoux B. Synlett 1990; 547
    • 6c Frantz DE, Fässler R, Carreira EM. J. Am. Chem. Soc. 2000; 122: 1806
    • 6d Sasaki H, Boyall D, Carreira EM. Helv. Chim. Acta 2001; 84: 964
    • 6e Tan L, Chen C.-Y, Tillyer RD, Grabowski EJ. J, Reider PJ. Angew. Chem. Int. Ed. 1999; 38: 711
  • 8 Huang B, Yao X, Li C.-J. Adv. Synth. Catal. 2006; 348: 1528
  • 9 Tzalis D, Knochel P. Angew. Chem. Int. Ed. 1999; 38: 1463
  • 10 Pereshivko OP, Peshkov VA, Van der Eycken EV. Org. Lett. 2010; 12: 2638
  • 11 Boyall D, Lopez F, Sasaki H, Frantz DE, Carreira EM. Org. Lett. 2000; 2: 4233
  • 12 Sato I, Saito T, Soai K. Chem. Commun. 2000; 2471
  • 13 Xu Z, Chen C, Xu J, Miao M, Yan W, Wang R. Org. Lett. 2004; 6: 1193
    • 14a Ried W, Suarez-Rivero E. Chem. Ber. 1963; 96: 1475
    • 14b Chen G, Wang Y, Gao S, He H.-P, Li S.-L, Zhang J.-X, Ding J, Hao X.-J. J. Heterocycl. Chem. 2009; 46: 217
    • 14c Fu X.-P, Liu L, Wang D, Chena Y.-J, Li C.-J. Green Chem. 2011; 13: 549
  • 15 Peddibhotla S. Curr. Bioact. Compd. 2009; 5: 20 ; and references cited therein
  • 16 Boechat N, Kover WB, Bongertz V, Bastos MM, Romeiro NC, Azevedo ML. G, Wollinger W. Med. Chem. 2007; 3: 533