ChemInform Abstract: The Use of Formamidine Protection for the Derivatization of Aminobenzoic Acids

Autor:	W. Martin Rennells, Lisa H. Peterson, Paul Zhichkin, Catherine M. Beer
Rok vydání:	2009
Předmět:	chemistry.chemical_compound Chemistry Triazole derivatives Organic chemistry ETHYLENEDIAMINE DERIVATIVES General Medicine Derivatization
Zdroj:	ChemInform. 40
ISSN:	1522-2667 0931-7597
Popis:	N,N-Dimethylformamidine and novel N,N-diisopropylformamidine protecting groups were used to carry out a one-pot conversion of aminobenzoic acids into the corresponding amides. General conditions for an in situ transformation of aminobenzoic acids and their heterocyclic analogues into the corresponding formamidine-protected acid chlorides were developed. These chlorides were used in reactions with amines, including poorly reactive anilines. The protected amides were then smoothly deprotected by heating with ethylenediamine derivatives, resulting in a general procedure for the one-pot transformation of aminobenzoic acids into their amides. Our one-pot procedure was successfully applied to the preparation of several compounds of pharmaceutical interest.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::94ed01e686845d4db4665a808b76c22b https://doi.org/10.1002/chin.200915080 Zobrazit plný text záznamu Plný text