Asymmetric Synthesis of Biologically Active Materials

生物活性材料的不对称合成

• 批准号: 6321476
• 负责人: SCOTT G. NELSON
• 金额: $ 21.42万
• 依托单位: UNIVERSITY OF PITTSBURGH AT PITTSBURGH
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-09-01 至 2005-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6321476
• 关键词: antineoplastics; antiviral agents; chemical bond; chemical synthesis; cyclic peptides; drug design /synthesis /production; inhibitor /antagonist; integrins; organic chemicals; stereochemistry

DESCRIPTION: (Applicant's Description) Our principle goal during the tenure of this grant will be the development of new catalyzed organic reactions for the stereospecific assemblage of C-C bond with broad, applications to the synthesis of a variety of target compounds possessing pharmacological activity. The reaction technology under development is specifically designed to address fundamental C-C bond forming reactions that are generally applicable to complex molecule synthesis and the preparation of important chemical building blocks in the context of industrial or medicinal chemistry synthesis activities. Catalyzed asymmetric acyl chloride-aldehyde cyclocondensations developed in our laboratories are further developed as versatile reaction technology for asymmetric organic synthesis. This methodology will be refined and developed in the context of the total synthesis of naturally occurring materials that express potent anticancer and antiviral activities, including amphidinolide B, rhazinilam, and motuporin. Moreover, a family of unique optically active Al(III)-based Lewis acids will be developed as bifunctional Lewis acidic-Lewis basic catalysts with applications to a variety of asymmetric C-C bond constructions. An economical and operationally simple synthesis of highly enantiomerically enriched beta-amino acids is also exploited in an efficient approach to the synthesis of beta-peptides and the preparation of cyclic beta-peptide structures designed to function as integrin receptor antagonists.

（申请人描述）在此资助期间，我们的主要目标是开发新的催化有机反应