ORGN 788 |
| Roland E. Dolle, Blanca Martinez-Teipel, and Calum MacLeod. Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341 |
| Amine derivatization is the most widely employed transformation in combinatorial and medicinal chemistry. Numerous streamlined synthesis protocols are available to generate collections of amides, sulfonamides, ureas and amines from primary and secondary amines. These protocols yield acyclic derivatives. Of equal importance is the rapid access to cyclic derivatives. Single–step amine annulation chemistries have been developed as part of the title technology platform to address this void. This first disclosure takes an in–depth look at a novel series of SPAnTM reagents that transform primary amines into diverse arrays of C(O)NR–containing heterocycles. The reagents are well suited for establishing nascent structure–activity relationships in biologically active lead compounds. |
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Combinatorial, Parallel, and Solid-Phase Chemistry
1:00 PM-5:00 PM, Thursday, August 26, 2004 Pennsylvania Convention Center -- 202B, Oral
Division of Organic Chemistry |