Synthesis 2016; 48(08): 1226-1234
DOI: 10.1055/s-0035-1561355
paper
© Georg Thieme Verlag Stuttgart · New York

Synthesis of Novel Hydroxymethyl-Substituted Fused Heterocycles

Authors

  • Jane L. Holmes*

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Lynsie Almeida

    b   AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
  • Bernard Barlaam

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Rosemary A. Croft

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Allan P. Dishington

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Laksmaiah Gingipalli

    b   AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
  • Lorraine A. Hassall

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Janet L. Hawkins

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Stephanos Ioannidis

    b   AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
  • Jeffrey W. Johannes

    b   AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
  • Thomas M. McGuire*

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Jane E. Moore

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Anil Patel

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Kurt G. Pike

    a   AstraZeneca R&D Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK   Email: Thomas.McGuire@astrazeneca.com
  • Timothy Pontz

    b   AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
  • Xiaoyun Wu

    b   AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
  • Tao Wang

    b   AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
  • Hai-Jun Zhang

    b   AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
  • Xiaolan Zheng

    b   AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
Further Information

Publication History

Received: 17 December 2015

Accepted after revision: 08 January 2016

Publication Date:
18 February 2016 (online)


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◊ Current address: AstraZeneca R&D, Darwin Building (310), Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, UK

Abstract

Examples of hydroxymethylated analogues of heteroaryl cores such as quinazolin-4-ones, isoquinolin-1(2H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, chromen-4-ones and pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones are sparse or non-existent in the scientific literature. We have demonstrated that such compounds are accessible by using standard procedures from readily available raw materials.

Supporting Information