A simple, efficient and eco-friendly protocol has been developed for the deprotection of N-Boc on structurally diverse amines. Selective removal of N-Boc groups was achieved with excellent yields using water around reflux temperatures. In the absence of any additional reagents, this method represents a reasonable alternative to previously reported deprotection procedures.
A facile and versatile method for acylation of structurally diverse amines and sulfonamides under focused ultrasonic irradiation in catalyst-free and solvent-free conditions is reported. There are several advantages to this approach such as simple and easier workup conditions, small amount of time and high yielding. The acylation reaction was carried out with acetic anhydride. All structures of synthesized products have been identified by NMR and mass spectroscopy.
pounds. -The preparation of chiral cyclosulfamides (VII) is performed starting from amino esters (I). Benzoylation of (I), followed by reduction and chlorination yield the chiral 1-substituted N-benzyl chloroethylamine hydrochlorides (V). Sulfonylation of (V) by N-Boc sulfamoyl chloride (VI) under alkaline conditions causes spontaneous cyclization into chiral thiadiazolidine dioxides (VII). Regioselective deprotection of the five-membered cyclosulfamides (VII) is achieved by using the fusion method, consisting of heating (VII) in the presence of a catalytic quantity of iodine under reduced pressure. -(NADIA, K.; MALIKA, B.; NAWEL, K.; MEDYAZID, B.; ZINE, R.; AOUF*, N.-E.; J.
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