Syntheses of brostallicin starting from distamycin A

Autor:	Marcella Nesi, Italo Beria
Rok vydání:	2002
Předmět:	Brostallicin Organic Chemistry General Medicine Combinatorial chemistry Biochemistry chemistry.chemical_compound chemistry Reagent Amide Drug Discovery Functional group Side chain Organic chemistry A-DNA Imide Curtius rearrangement
Zdroj:	Tetrahedron Letters. 43:7323-7327
ISSN:	0040-4039
DOI:	10.1016/s0040-4039(02)01733-1
Popis:	Two syntheses of brostallicin, a DNA minor groove binder now undergoing phase II studies, starting from distamycin A are described. One approach is based upon the selective hydrolysis via imide activation of the C-terminus amide. Besides employing traditional solution-phase synthesis, the convenient use of a polymer-supported reagent is also discussed. The other one is based upon the Curtius rearrangement of the C-terminus side chain of a convenient intermediate, easily prepared in two steps by straightforward functional group manipulation of distamycin A.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72330218c56a18e52a8f5aed3ba55956 https://doi.org/10.1016/s0040-4039(02)01733-1 Zobrazit plný text záznamu Full Text from ScienceDirect