Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer’s Disease
1
WuXi AppTec (Shanghai)
Pharmaceutical Co., Ltd., 288 Fute
Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China
|
Publication type: Journal Article
Publication date: 2016-11-04
scimago Q1
wos Q1
SJR: 1.235
CiteScore: 8.7
Impact factor: 5.0
ISSN: 15237060, 15237052
PubMed ID:
27934506
Organic Chemistry
Biochemistry
Physical and Theoretical Chemistry
Abstract
Verubecestat is an inhibitor of β-secretase being evaluated for the treatment of Alzheimer's disease. The first-generation route relies on an amide coupling with a functionalized aniline, the preparation of which introduces synthetic inefficiencies. The second-generation route replaces this with a copper-catalyzed C-N coupling, allowing for more direct access to the target. Other features of the new route include a diastereoselective Mannich-type addition into an Ellman sulfinyl ketimine and a late-stage guanidinylation.
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Metrics
37
Total citations:
37
Citations from 2025:
1
(2.7%)
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MLA
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GOST
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Thaisrivongs D. A. et al. Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer’s Disease // Organic Letters. 2016. Vol. 18. No. 22. pp. 5780-5783.
GOST all authors (up to 50)
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Lu C. Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer’s Disease // Organic Letters. 2016. Vol. 18. No. 22. pp. 5780-5783.
Cite this
RIS
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TY - JOUR
DO - 10.1021/acs.orglett.6b01793
UR - https://doi.org/10.1021/acs.orglett.6b01793
TI - Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer’s Disease
T2 - Organic Letters
AU - Lu, Chen
PY - 2016
DA - 2016/11/04
PB - American Chemical Society (ACS)
SP - 5780-5783
IS - 22
VL - 18
PMID - 27934506
SN - 1523-7060
SN - 1523-7052
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2016_Thaisrivongs,
author = {Chen Lu},
title = {Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer’s Disease},
journal = {Organic Letters},
year = {2016},
volume = {18},
publisher = {American Chemical Society (ACS)},
month = {nov},
url = {https://doi.org/10.1021/acs.orglett.6b01793},
number = {22},
pages = {5780--5783},
doi = {10.1021/acs.orglett.6b01793}
}
Cite this
MLA
Copy
Thaisrivongs, David A., et al. “Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer’s Disease.” Organic Letters, vol. 18, no. 22, Nov. 2016, pp. 5780-5783. https://doi.org/10.1021/acs.orglett.6b01793.