Document Detail


Efficient synthesis of 3-aminocyclobut-2-en-1-ones: squaramide surrogates as potent VLA-4 antagonists.
MedLine Citation:
PMID:  12816444     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A novel series of uniquely functionalized 3-aminocyclobut-2-en-1-ones has been prepared by facile condensation of a variety of cyclobuta-1,3-diones with a phenylalanine-derived primary amine. These systems subsequently lend themselves to substitution at C-2 by reaction with a variety of electrophilic reagents including N-halosuccinimides, sulfenyl chlorides, and Eschenmoser's salt. Compounds from this novel series are potent antagonists of VLA-4. [reaction: see text]
Authors:
Stephen Brand; Benjamin C de Candole; Julien A Brown
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Organic letters     Volume:  5     ISSN:  1523-7060     ISO Abbreviation:  Org. Lett.     Publication Date:  2003 Jun 
Date Detail:
Created Date:  2003-06-20     Completed Date:  2003-11-24     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  100890393     Medline TA:  Org Lett     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2343-6     Citation Subset:  IM    
Affiliation:
Medicinal Chemistry, Celltech Group plc, 216 Bath Road, Slough SL1 4EN, UK.
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MeSH Terms
Descriptor/Qualifier:
Cyclobutanes / chemistry*,  pharmacology*
Indicators and Reagents
Integrin alpha4beta1 / antagonists & inhibitors*
Ketones / chemical synthesis*,  pharmacology*
Phenylalanine / analogs & derivatives
Chemical
Reg. No./Substance:
0/Cyclobutanes; 0/Indicators and Reagents; 0/Integrin alpha4beta1; 0/Ketones; 63-91-2/Phenylalanine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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