Abstract
An effective approach for amino protection and construction of a seven-membered ring has been developed. The method uses imidazolium chloride to carry out the Michael addition reaction at low temperatures and perform amino deprotection or construction of a seven-membered ring at high temperatures.
Highlights
Many pharmaceutical intermediates or active molecules often contain amino groups
When we began to study the reaction of o-phenylenediamine with N,N-dimethylacrylamide catalyzed by imidazolium chloride to construct a seven-membered ring [16,17,18], we found that the Molecules 2019, 24, 4224; doi:10.3390/molecules24234224
Imidazolium chloride as a green catalyst. Based on on these these results, results, we we propose propose using using imidazolium imidazolium hydrochloride hydrochloride to to catalyze catalyze the the Michael
Summary
Many pharmaceutical intermediates or active molecules often contain amino groups. The amino groups are unstable and oxidized. The protection of amino groups is often needed in the process of drug synthesis. Methods of amino functional group protection have been reported by related literatures or patents [1]. Functional groups were protected via amines reacting with CBZ-Cl [2,3], (Boc) O [4,5,6], Fmoc-Cl [7], TFA [8,9] and Alloc-Cl [10] in the presence of inorganic bases. We have found that bases are mainly used as a promoter. Jadhav et al [11]
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