volume 19 issue 7 pages 865-871

Asymmetric Fluorination Approach to the Scalable Synthesis of a SYK Inhibitor

Neil R Curtis 1
Suzanne H Davies 1
Matthew Gray 1
Stuart G Leach 1
Ross A Mckie 1
Lois E Vernon 1
Andrew J. Walkington 1
Publication typeJournal Article
Publication date2015-06-25
scimago Q1
wos Q1
SJR0.865
CiteScore5.4
Impact factor3.5
ISSN10836160, 1520586X
Organic Chemistry
Physical and Theoretical Chemistry
Abstract
A large-scale process for the synthesis of SYK inhibitor 1 has been developed and used to deliver multi-kilogram yields of this active pharmaceutical ingredient. Integral to the scalable process is a combined chiral auxiliary and chiral catalyst mediated diastereoselective fluorination. Safe processes for BH3·DMS-mediated reduction of ester and amide functions and azide introduction, and a robust Suzuki–Miyaura coupling of a pyrazyl boronate with chloronapthyridine, are described.
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GOST |
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GOST Copy
Curtis N. R. et al. Asymmetric Fluorination Approach to the Scalable Synthesis of a SYK Inhibitor // Organic Process Research and Development. 2015. Vol. 19. No. 7. pp. 865-871.
GOST all authors (up to 50) Copy
Curtis N. R., Davies S. H., Gray M., Leach S. G., Mckie R. A., Vernon L. E., Walkington A. J. Asymmetric Fluorination Approach to the Scalable Synthesis of a SYK Inhibitor // Organic Process Research and Development. 2015. Vol. 19. No. 7. pp. 865-871.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1021/acs.oprd.5b00131
UR - https://doi.org/10.1021/acs.oprd.5b00131
TI - Asymmetric Fluorination Approach to the Scalable Synthesis of a SYK Inhibitor
T2 - Organic Process Research and Development
AU - Curtis, Neil R
AU - Davies, Suzanne H
AU - Gray, Matthew
AU - Leach, Stuart G
AU - Mckie, Ross A
AU - Vernon, Lois E
AU - Walkington, Andrew J.
PY - 2015
DA - 2015/06/25
PB - American Chemical Society (ACS)
SP - 865-871
IS - 7
VL - 19
SN - 1083-6160
SN - 1520-586X
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2015_Curtis,
author = {Neil R Curtis and Suzanne H Davies and Matthew Gray and Stuart G Leach and Ross A Mckie and Lois E Vernon and Andrew J. Walkington},
title = {Asymmetric Fluorination Approach to the Scalable Synthesis of a SYK Inhibitor},
journal = {Organic Process Research and Development},
year = {2015},
volume = {19},
publisher = {American Chemical Society (ACS)},
month = {jun},
url = {https://doi.org/10.1021/acs.oprd.5b00131},
number = {7},
pages = {865--871},
doi = {10.1021/acs.oprd.5b00131}
}
MLA
Cite this
MLA Copy
Curtis, Neil R., et al. “Asymmetric Fluorination Approach to the Scalable Synthesis of a SYK Inhibitor.” Organic Process Research and Development, vol. 19, no. 7, Jun. 2015, pp. 865-871. https://doi.org/10.1021/acs.oprd.5b00131.