Methods for preparation of macrocyclic molecules and macrocyclic molecules prepared thereby

US7279304B2 · kind B2 · utility

Assignee

• President and Fellows of Harvard College · US

Inventors

• Christopher Walsh · Wellesley, US
• John Trauger · Cambridge, US
• Rahul Kohli · Cambridge, US
• Michael D. Burkart · Boston, US
• Mohammed A. Maraheil · Marburg, DE
• Henning Mootz · Marburg, DE
• Dirk Schwarzer · Marburg, DE

Key dates

• Filing date: Dec 15, 2001
• Grant date: Oct 9, 2007
• Expiry date: Dec 15, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K7/66
• WIPO field: Biotechnology
• WIPO sector: Chemistry

Abstract

The preparation of macrocyclic molecules from linear, synthetic thioester precursors is disclosed. An excised thioesterase domain isolated from either a polyketide synthases (PKS) or non-ribosomal peptide synthetases (NRPS) multido system catalyzes the cyclization reaction. Thioester substrates also are described that are efficiently cyclized by the method of the present invention. Additionally, macrocyclic molecules, including macrolactones and macrolactams, that are prepared by the macrocyclization methods of the invention are described.