218631-50-6Relevant articles and documents
Substituted benzimidazole derivatives
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Paragraph 0054; 0055; 0056; 0117; 0118; 0119, (2018/01/09)
The invention belongs to the field of pharmaceutical chemistry, particularly relates to substituted benzimidazole derivatives as well as a preparation method and pharmaceutical composition thereof and further relates to an application of the substituted b
The use of formamidine protection for the derivatization of aminobenzoic acids
Zhichkin, Paul E.,Peterson, Lisa H.,Beer, Catherine M.,Rennells, W. Martin
supporting information; experimental part, p. 8954 - 8959 (2009/04/11)
(Chemical Equation Presented) 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.