Source:http://linkedlifedata.com/resource/pubmed/id/19532999
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
13
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pubmed:dateCreated |
2009-6-17
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pubmed:abstractText |
A rapid and versatile one-pot, 2 x 10 min microwave protocol for the preparation of N-1 and C-6 decorated 3,5-dichloro-2(1H)-pyrazinones was developed. Comparable reaction sequences using classical conditions require about 1-2 days of heating. The alpha-aminonitrile was first generated in a Strecker reaction and thereafter cyclized under microwave heating. The microwave approach developed offers the possibility of efficiently generating and utilizing functionalized 3-amino-5-chloro-2(1H)-pyrazinone-N-1-carboxylic acids as beta-strand inducing core structures in a medicinal chemistry context. To illustrate the usefulness of the method, the synthesis of two novel 2(1H)-pyrazinone-containing Hepatitis C virus NS3 protease inhibitors is reported.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1477-0539
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
7
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pubmed:volume |
7
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2809-15
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pubmed:meshHeading |
pubmed-meshheading:19532999-Enzyme Inhibitors,
pubmed-meshheading:19532999-Hepacivirus,
pubmed-meshheading:19532999-Microwaves,
pubmed-meshheading:19532999-Molecular Structure,
pubmed-meshheading:19532999-Pyrazines,
pubmed-meshheading:19532999-Stereoisomerism,
pubmed-meshheading:19532999-Structure-Activity Relationship,
pubmed-meshheading:19532999-Viral Nonstructural Proteins
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pubmed:year |
2009
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pubmed:articleTitle |
A straightforward microwave method for rapid synthesis of N-1, C-6 functionalized 3,5-dichloro-2(1H)-pyrazinones.
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pubmed:affiliation |
Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala Biomedical Centre, Uppsala University, Box 574, SE-751 23, Uppsala, Sweden.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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