Tentoxin as a scaffold for drug discovery. Total solid-phase synthesis of tentoxin and a library of analogues

Organic Letters

Volumn 5, Issue 12, 2003, Pages 2115-2118

  Jiménez, Jose C ^a   Chavarría, Bibiana ^a   López Macià, Àngel ^a,b   Royo, Miriam ^a   Giralt, Ernest ^a   Albericio, Fernando ^a  

^a UNIVERSITY OF BARCELONA   (Spain)

^b PHARMAMAR S A   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

PLANT TOXIN; TENTOXIN; UNCLASSIFIED DRUG;

ALKYLATION; AMINO ACID SEQUENCE; ARTICLE; CHEMICAL STRUCTURE; DRUG DESIGN; DRUG IDENTIFICATION; DRUG SYNTHESIS; SOLID;

AMINO ACID SEQUENCE; COMBINATORIAL CHEMISTRY TECHNIQUES; MYCOTOXINS; PEPTIDES, CYCLIC; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0141742497     PISSN: 15237060     EISSN: None     Source Type: Journal    
DOI: 10.1021/ol0345273     Document Type: Article

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36. Although tentoxin and its analogues were obtained after cyclization with excellent purity, similar to that shown by tentoxin (HPLC profile X, Scheme 1), further purification was carried out in all cases by reversed-phase HPLC to give compounds with a purity greater than 95%.
37. 3 (10 equiv) in anhydrous DCM (3 x 15 min) under an Ar atmosphere.