Synthesis 2012; 44(13): 1983-1992
DOI: 10.1055/s-0031-1290969
paper
© Georg Thieme Verlag Stuttgart · New York

Diastereocontrol in the Synthesis of 2,3,4-Trisubstituted Pyrrolidines and Tetrahydrofurans via a Palladium(II)-Catalyzed Three-Component Coupling Reaction

Sandeep Raikar
Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA
Center of Excellence in Chemical Methodologies and Library Development, University of Kansas, 2034 Becker Drive, Shankel Structural Biology Center, West Campus, Lawrence, KS 66047, USA, Fax: +1(785)8645396   Email: hmalina@ku.edu
,
Benoy Kumar Pal
Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA
Center of Excellence in Chemical Methodologies and Library Development, University of Kansas, 2034 Becker Drive, Shankel Structural Biology Center, West Campus, Lawrence, KS 66047, USA, Fax: +1(785)8645396   Email: hmalina@ku.edu
,
Helena C. Malinakova*
Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA
Center of Excellence in Chemical Methodologies and Library Development, University of Kansas, 2034 Becker Drive, Shankel Structural Biology Center, West Campus, Lawrence, KS 66047, USA, Fax: +1(785)8645396   Email: hmalina@ku.edu
› Author Affiliations
Further Information

Publication History

Received: 31 January 2012

Accepted after revision: 23 March 2012

Publication Date:
05 June 2012 (online)


Abstract

The synthesis of trisubstituted pyrrolidines and tetrahydrofurans from boronic acids, allenes, and imines or aldehydes via a five- and a three-step protocol, respectively, is described. The assignment­ of the relative stereochemistry in the pyrrolidines and tetrahydrofurans confirmed the mechanistically significant stereochemical divergence of the palladium-catalyzed three-component coupling reaction. The methodology is applicable to the preparation of combinatorial libraries of pyrrolidines related to pharmaceutical agents and bioactive natural products.

Supporting Information

 
  • References

    • 1a Jae H.-S, Winn M, von Geldern TW, Sorensen BK, Chiou WJ, Nguyen B, Marsh KC, Opgenorth TJ. J. Med. Chem. 2001; 44: 3978
    • 1b Yang B.-H, Zhang W.-D, Liu R.-H, Li T.-Z, Zhang C, Zhou Y, Su J. J. Nat. Prod. 2005; 68: 1175
    • 1c Lin SL, Liu X.-H, Shen Y.-H, Li H.-L, Shan L, Liu R.-H, Xu X.-K, Zhang W.-D, Wang H. J. Nat. Prod. 2010; 73: 632
  • 2 Slater MJ, Amphlett EM, Andrews DM, Bravi G, Burton G, Cheasty AG, Corfield JA, Ellis MR, Fenwick RH, Fernandes S, Guidetti R, Haigh D, Hartley CD, Howes PD, Jackson DL, Jarvest RL, Lovegrove VL. H, Medhurst KJ, Parry NR, Price H, Shah P, Singh OM. P, Stocker R, Thommes P, Wilkinson C, Wonacott A. J. Med. Chem. 2007; 50: 897
  • 3 Baldwin JE, Fryer AM, Pritchard GJ. J. Org. Chem. 2001; 66: 2588
    • 4a Chen C, Li X, Schreiber SL. J. Am. Chem. Soc. 2003; 125: 10174
    • 4b Scott ME, Han W, Lautens M. Org. Lett. 2004; 6: 3309
    • 4c Pohlhaus PD, Sanders SD, Parsons AT, Li W, Johnson JS. J. Am. Chem. Soc. 2008; 130: 8642
    • 4d Chaulagain MR, Aron ZD. J. Org. Chem. 2010; 75: 8271
  • 5 Barker G, McGrath JL, Klapars A, Stead A, Stead D, Zhou G, Campos KR, O’Brien P. J. Org. Chem. 2011; 76: 5936
    • 6a Bueno ND, Jimenez A, Pedregal C, Vidal P. Tetrahedron Lett. 2006; 17: 2489
    • 6b Yazici A, Pyne SG. Synthesis 2009; 513
    • 6c Peixoto S, Nguyen TM, Crich D, Delpech B, Marazano C. Org. Lett. 2010; 12: 4760
    • 7a Paderes MC, Chemler SR. Org. Lett. 2009; 11: 1915
    • 7b Komsta Z, Barbasiewicz M, Makosza M. J. Org. Chem. 2010; 75: 3251
    • 7c Zhou L, Chen J, Tan CK, Yeung Y.-Y. J. Am. Chem. Soc. 2011; 133: 9164
    • 7d Kotland A, Accadbled F, Robeyns K, Behr J.-B. J. Org. Chem. 2011; 76: 4094
  • 9 Hopkins CD, Malinakova HC. Org. Lett. 2004; 6: 2221
    • 10a Murphy MM, Schullek JR, Gordon EM, Gallop MA. J. Am. Chem. Soc. 1995; 117: 7029
    • 10b Kumar A, Gupta G, Srivastava S. J. Comb. Chem. 2010; 12: 458
    • 10c Liu H, Dou G, Shi D. J. Comb. Chem. 2010; 12: 292
    • 11a An H, Cook PD. Chem. Rev. 2000; 100: 3311
    • 11b Sunderhaus JD, Martin SF. Chem.–Eur. J. 2009; 15: 1300
    • 11c Ganem B. Acc. Chem. Res. 2009; 42: 463
    • 11d See also ref. 4d
  • 12 Hopkins CD. Ph.D. Thesis. The University of Kansas; USA: 2007
  • 13 Verkade JM. M, van Hemert LJ. C, Quaedflieg PJ. L. M, Alsters PL, van Delft FL, Rutjes FP. J. T. Tetrahedron Lett. 2006; 47: 8109
    • 14a Kronenthal DR, Han CY, Taylor MK. J. Org. Chem. 1982; 47: 2765
    • 14b Hasegawa M, Taniyama D, Tomioka K. Tetrahedron 2000; 56: 10153
    • 14c Overman LE, Owen CE, Pavan MM. Org. Lett. 2003; 5: 1809
    • 14d Hata S, Iguchi M, Iwasawa T, Yamada K.-I, Tomioka K. Org. Lett. 2004; 6: 1721
    • 14e Marin SD. L, Martens T, Mioskowski C, Royer J. J. Org. Chem. 2005; 70: 10592
    • 15a Maligres PE, Waters MM, Lee J, Reamer RA, Askin D, Ashwood MS, Cameron M. J. Org. Chem. 2002; 67: 1093
    • 15b Sajjadi Z, Lubell WD. J. Pept. Res. 2005; 65: 298
  • 16 Burkhardt ER, Matos K. Chem. Rev. 2006; 106: 2617
  • 17 Bieber LW, de Araujo MC. F. Molecules 2002; 7: 902
  • 18 Lucas BS, Luther LM, Burke SD. Org. Lett. 2004; 6: 2965
  • 19 Rujirawanich J, Gallagher T. Org. Lett. 2009; 11: 5494
  • 20 Prakash GK. S, Do C, Wang F, Mathew T, Olah GA. Synthesis 2010; 1891
    • 21a Still WC, Barrish JC. J. Am. Chem. Soc. 1983; 105: 2487
    • 21b Loiseleur O, Koch G, Wagner T. Org. Process Res. Dev. 2004; 8: 597
    • 22a Houk KN, Rondan NG, Wu YD, Metz JT, Paddon-Row MN. Tetrahedron 1984; 40: 2257
    • 22b Hoffmann RW. Chem. Rev. 1989; 89: 1841
  • 23 Evans DA, Ratz AM, Huff BE, Sheppard GS. J. Am. Chem. Soc. 1995; 117: 3448
  • 24 X-ray crystallographic data were deposited at the Cambridge Crystallographic Data Centre, CCDC number 858605