Source:http://linkedlifedata.com/resource/pubmed/id/18590336
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
15
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pubmed:dateCreated |
2008-7-25
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pubmed:abstractText |
Two novel routes have been developed to the (3 R,6 S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one 2 of the CGRP receptor antagonist clinical candidate telcagepant (MK-0974, 1). The first employs a ring-closing metathesis of the styrene 7 as the key reaction, while the second makes use of a highly diastereoselective Hayashi-Miyaura Rh-catalyzed arylboronic acid addition to nitroalkene 16. The latter route has been implemented to produce multigram quantities of telcagepant for extensive preclinical evaluation.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Azepines,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/N-(6-(2,3-difluorophenyl)-2-oxo-1-(2...,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Calcitonin Gene-Related...
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1523-7060
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
10
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3235-8
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pubmed:meshHeading | |
pubmed:year |
2008
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pubmed:articleTitle |
Synthesis of the (3R,6S)-3-amino-6-(2,3-difluorophenyl)azepan-2-one of telcagepant (MK-0974), a calcitonin gene-related peptide receptor antagonist for the treatment of migraine headache.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA. christopher_burgey@merck.com
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pubmed:publicationType |
Journal Article
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