Multigram Synthesis of Tetrasubstituted Dihydrobenzofuran GSK973 Enabled by High-Throughput Experimentation and a Claisen Rearrangement in Flow-Reference-Cited by-同舟云学术

Multigram Synthesis of Tetrasubstituted Dihydrobenzofuran GSK973 Enabled by High-Throughput Experimentation and a Claisen Rearrangement in Flow

Published:2022-01-24 Issue:2 Volume:26 Page:365-379
ISSN:1083-6160
Container-title:Organic Process Research & Development
language:en
Short-container-title:Org. Process Res. Dev.

Author:

Alder Catherine M.¹^ORCID,Gray Matthew²,Huff Chelsea A.³,Manning Calvin O.²,Preston Alex⁴^ORCID,Rushworth Philip²,Shuster Leanna E.⁵,Watson Robert J.⁴,Wheelhouse Katherine M. P.²^ORCID,Williams Glynn D.²,Demont Emmanuel H.⁴^ORCID

Affiliation:

1. UK Green Chemistry, GlaxoSmithKline, Stevenage, Hertfordshire SG1 2NY, U.K.

2. API Chemistry U.K, GlaxoSmithKline, Stevenage, Hertfordshire SG1 2NY, U.K.

3. Discovery Automation Platform Chemistry, GlaxoSmithKline, 1250 S. Collegeville Rd, Collegeville, Pennsylvania 19426, United States

4. Epigenetics Discovery Performance Unit, Immunoinflammation Therapy Area Unit, Medicines Research Centre, GlaxoSmithKline, Stevenage, Hertfordshire SG1 2NY, U.K.

5. US Green Chemistry, GlaxoSmithKline, 1250 S. Collegeville Rd, Collegeville, Pennsylvania 19426, United States

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.1c00422

Reference22 articles.

1. Targeting bromodomains: epigenetic readers of lysine acetylation

2. BET inhibitors: a novel epigenetic approach

3. Bromodomain inhibitors a decade later: a promise unfulfilled?

4. Atkinson, S. J.; Demont, E. H.; Harrison, L. A.; Atkinson, S. J.; Demont, E. H.; Harrison, L. A.; Preston, A. G.; Seal, J. T.; Wall, I. D.; Watson, R. J.; Woolven, J. M. Benzo[b]furans as bromodomain inhibitors. WO 2017174620 A1, 2017.

5. The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor

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3. Correction to “Multigram Synthesis of Tetrasubstituted Dihydrobenzofuran GSK973 Enabled by High-Throughput Experimentation and a Claisen Rearrangement in Flow”;Organic Process Research & Development;2022-03-10