ORGN 928 |
| Amino heterocycles are ubiquitous and among the greatest biological and pharmaceutical compounds of interest. The synthesis of such, however, remains challenging. Multiple steps are routinely required, including protection of functional groups if present, activation of corresponding cyclic amide or urea moieties often under harsh acidic conditions, followed by an SNAr displacement and finally deprotection of the functional groups to generate the desired products. The overall efficiency of these multi-steps syntheses is frequently unsatisfactory. Destruction of acid-labile functional groups and loss of protecting groups are common problems encountered in these transformations. A practical and efficient one-step amination of cyclic amides and cyclic ureas has been developed. The superior compatibility to many functional groups, high efficiency for the synthesis of many biologically important natural and unnatural products, and preliminary mechanistic aspects of this new methodology will be discussed.
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Heterocycles and Aromatics
1:00 PM-4:40 PM, Thursday, 14 September 2006 Moscone Center -- Room 135, Oral
Division of Organic Chemistry |
