ORGN 730 |
| Since the first report on the preparation of amidines (Pinner's synthesis) in connection with imidate chemistry more than a century ago, there is still an active interest in this area because of the synthetic and biological potential of this functional group. Our interest in this stems from our recent effort to develop the synthesis of an active pharmaceutical ingredient. The current synthetic sequences called for more efficient synthesis of the corresponding acetimidine. Thus, a highly efficient reagent for synthesis of acetamidines from amine was developed. These reagents are highly versatile and demonstrate wider substrate scope. Also, appropriate choice of reaction conditions allows the easy isolation of crystalline salts (inorganic or organic) depending on the nature of the substrate. Interestingly, highly hindered or poorly nucleophilic amine substrates that are obstinate towards other reagents and conditions were also efficiently converted to the product. The application of this reagent in a novel approach designed for direct synthesis of substituted aminopyrazoles will be discussed. |
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Combinatorial, Parallel and Process Chemistry, Heterocycles, Aromatics, New Reactions and Methodology
8:00 PM-10:00 PM, Wednesday, August 22, 2007 BCEC -- Exhibit Hall - B2, Poster
Division of Organic Chemistry |