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Total Synthesis Highlights - Organic Chemistry Portal

A multi-gram total synthesis of discodermolide (133) was completed in order for Novartis to begin Phase I clinical trials.

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For example, the syntheses of phorboxazole A, spongistatin 1 and discodermolide (the latter two on gram scale) inspired the development of new methods such as the Petasis-Ferrier Union/Rearrangement, now widely applicable to natural products containing cis-tetrahydropyran rings, and multicomponent Anion Relay Chemistry (ARC), a new tactic that now permits the “one-pot” union of multiple fragments by controlling, in precise fashion, the migration of negative charge in a molecular array as the structural complexity increases in a highly convergent manner.

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and and and and and (2002)Discodermolide/Dictyostatin Hybrids: Synthesis and Biological Evaluation. Organic Letters, 4 (25). 4443 - 4446. ISSN 1523-7060

Discovery and development of tubulin inhibitors - …

(Matrix Presented) Two hybrid analogues of discodermolide and dictyostatin (3, 26) have been designed and synthesized

(Matrix Presented) Two hybrid analogues of discodermolide and dictyostatin (3, 26) have been designed and synthesized. These are the first macrocyclic analogues of discodermolide and biological activities were evaluated and compared with linear discodermolide analogues.

(Matrix Presented) Two hybrid analogues of discodermolide and dictyostatin (3, 26) have been designed and synthesized. These are the first macrocyclic analogues of discodermolide and biological activities were evaluated and compared with linear discodermolide analogues.

Structure-Activity Relationships Analysis of ..

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  • 03/06/2017 · Structure-Activity Relationships Analysis of (+)-Discodermolide and the Synthesis of Precursors for Further Analogue Studies

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