This document discusses various conventional and new methods for amidation or amide bond formation, including: 1) Catalytic acylation of amines using a-hydroxyenones or activated carboxylates. 2) Nucleophilic carbene and HOAt catalyzed amide coupling using a Breslow intermediate. 3) Milstein's catalyst for converting alcohols to amides. 4) Pd-catalyzed aminocarbonylation of aryl bromides. 5) Amidation of thioacids with azides, isocyanates, or isothiocyanates. 6) Microwave assisted amidation by acylation with amine derivatives.

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Presented By :
Gurudutt Dubey
M.Tech. (Pharm.) I Semester
Department of Pharmaceutical Technology (Process Chemistry)
National Institute of Pharmaceutical Education and Research, Mohali, Punjab (India)

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Conventional method
Nature, 2011, 480, 471–479

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New acylation reactions of amines
Amidation by catalytic acylation of amines
Nature, 2011, 480, 471–479

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Nucleophilic Carbene and HOAt Catalyzed Amide Bond
Coupling
Mechanism:
J. Am. Chem. Soc. 2007, 129, 13797

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Catalytic amide formation with a-hydroxyenones as acylating
reagents
Chem. Commun. 2009, 4566–4568

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Mechanism:
Breslow intermediate

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Milstein’s catalyst for conversion of alcohols into amides
Chem. Soc. Rev., 2011, 40, 3405–3415

8. Metal catalytized oxidative amidation of amines8
Nature, 2011, 480, 471–479
Oxidative coupling of α-bromo nitroalkanes with amines

9. Amidation by catalytic generation of activated carboxylates
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Nature, 2011, 480, 471–479

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Chem. Soc. Rev., 2011, 40, 3405–3415
Pd-catalysed aminocarbonylation of aryl bromides

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Nature, 2011, 480, 471–479
Amidation of thioacids

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The Reaction of Thio Acids with Azides
J. Am. Chem. Soc. 2003, 125, 7754-7755
Polar solvent :
Nonpolar solvent :

13. 13 Reaction of Thioacids with Isocyanates and
Isothiocyanates
Org. Lett. 2009, 11, 3514-3517

14. Microwave assisted amidation by acylation with amine derivatives
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Nature, 2011, 480, 471–479

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