Document Detail


Highly efficient macrolactonization of ω-hydroxy acids using benzotriazole esters: synthesis of Sansalvamide A.
MedLine Citation:
PMID:  20820651     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A facile and mild macrolactonization reaction of ω-hydroxy acids was developed based on the transesterification of benzotriazole esters. Treatment of ω-hydroxy acids with 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC) and 1-hydroxy benzotriazole (HOBT) in chloroform provided macrolactones in excellent yields. The reactions were performed under basic, neutral and acidic conditions using N,N-dimethylaminopyridine (DMAP), tetrabutylammonium tetrafluoroborate (TBABF(4)) and BF(3)·Et(2)O, respectively. A calcined hydrotalcite was also used instead of DMAP. Finally, to test the scope of the protocol in the synthesis of biologically relevant macrolactones, the total synthesis of Sansalvamide A was carried out.
Authors:
José Antonio Morales-Serna; Ericka Sánchez; Ricardo Velázquez; Jorge Bernal; Eréndira García-Ríos; Rubén Gaviño; Guillermo Negrón-Silva; Jorge Cárdenas
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-08-31
Journal Detail:
Title:  Organic & biomolecular chemistry     Volume:  8     ISSN:  1477-0539     ISO Abbreviation:  Org. Biomol. Chem.     Publication Date:  2010 Nov 
Date Detail:
Created Date:  2010-10-14     Completed Date:  2011-02-01     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101154995     Medline TA:  Org Biomol Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  4940-8     Citation Subset:  IM    
Affiliation:
Instituto de Química, Universidad Nacional Autónoma de México Circuito Exterior, Ciudad Universitaria, Coyoacán 04510, México D.F., México.
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MeSH Terms
Descriptor/Qualifier:
Depsipeptides / chemical synthesis*,  chemistry
Esters / chemical synthesis,  chemistry
Hydroxy Acids / chemical synthesis,  chemistry*
Triazoles / chemical synthesis,  chemistry*
Chemical
Reg. No./Substance:
0/Depsipeptides; 0/Esters; 0/Hydroxy Acids; 0/Triazoles; 0/sansalvamide A; 27556-51-0/benzotriazole

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