Abstract
This Letter describes an efficient ring-closing metathesis approach to 2-chloro-4-amino-pyrimido[4,5-c]azepines and 2-chloro-4-amino-pyrimido[4,5-c]oxepines. These chlorides were applied to the synthesis of several potent γ-secretase modulators (GSMs).
Keywords:
2-Chloro-pyrimido[4,5-c]azepin-4-amine; 2-Chloro-pyrimido[4,5-c]oxepin-4-amine; Ring-closing metathesis (RCM); γ-Secretase modulator (GSM).
Copyright © 2016 Elsevier Ltd. All rights reserved.
MeSH terms
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Amyloid Precursor Protein Secretases / metabolism*
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Azepines / chemical synthesis
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Azepines / chemistry
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Azepines / pharmacology*
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Dose-Response Relationship, Drug
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Humans
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Molecular Structure
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Oxepins / chemical synthesis
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Oxepins / chemistry
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Oxepins / pharmacology*
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Structure-Activity Relationship
Substances
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Azepines
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Oxepins
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Pyrimidines
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Amyloid Precursor Protein Secretases