The shifting from “traditional” heteroaromatic design concepts in modern Medicinal Chemistry leads to increasing complexity of the synthesis of medicinally relevant molecules. The one of the best way for solving this problem is to apply in the synthesis the robust well-known procedures and achieves complexity by using the sophisticated, commercially available (if it is possible), building blocks. Therefore, the interest to 3D-shaped building blocks with high fractions of F(sp3)-hybridized carbon atoms continuously growth and now its synthesis become a part of the industry. Therefore, the procedures, which can effectively lead to the formation of targeted products in 10-100 gram scale become more and more demanded.<br/>We focused our attention on the elaboration of the effective multigram scale procedure for the synthesis of diverse 4-substituted 2,3-diketopyrrolidines. These ketones are a very rare class of organic compounds. For today there are only a few methods for obtaining such compounds in milligram scales. From the other hand these products have been a perspective building blocks for Medicinal Chemistry needs.<br/>In this report the synthetic methodology for the obtaining of 2,3-diketopyrrolidines is validated and optimized. The advantages and scope and limitation of the procedure are determined and will be discussed.

2,3-diketopirrolidines as perspective building blocks for medicinal chemistry: Synthesis and properties

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.