Process for the conversion of cyclic amines into lactams
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چکیده
Process for the conversion of cyclic amines into lactams" (2012).
منابع مشابه
N-Aryl Lactams by Regioselective Ozonation of N-Aryl Cyclic Amines
Ozonation of N-aryl-cyclic amines in organic solvents gave N-aryl-lactams regioselectively. In particular, 4-(4-aminophenyl)-morpolin-3-one, a key intermediate in the preparation of factor Xa inhibitors, was obtained in fair yields. The method represents an alternative approach for the lactamization of tertiary N-arylic substrates and is based on a "metal-free" introduction of the carbonyl func...
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Mesoporous MCM-41 silicas anchored with sulfonic acid (–SO3H) groups (denoted MSN-SA) via postsynthesis modification are very effective for the Beckman rearrangement. A simple and convenient procedure for conversion of a variety oximes to their corresponding amides and lactams has been developed. The reaction was carried out in the presence of MSN-SA as the catalyst. The best results for conver...
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Rapid and high yielding synthesis of medium ring lactams was made possible through the use of a benzoylurea auxiliary that serves to stabilize a cisoid amide conformation, facilitating cyclization. The auxiliary is released after activation under the mild conditions required to deprotect a primary amine, such as acidolysis of a Boc group in the examples given here. This methodology is a promisi...
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Two methods to reduce N-alkyl lactams to the corresponding cyclic amines using 9borabicyclo[3.3.1]nonane (9-BBN) and lithium aminoborohydride (LAB) reagents are reported. The lactam reductions required 2.2 molar equivalents of 9-BBN or 1.5 molar equivalents of LAB reagent and were complete within two hours in refluxing THF (65 °C). Reductions with these reagents are chemoselective and complemen...
متن کاملNucleophilic chiral amines as catalysts in asymmetric synthesis.
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