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Molecules 2013, 18(6), 6230-6268; doi:10.3390/molecules18066230

Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles

Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, 34 Rainbow Drive, Hilo, HI 96720, USA
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Received: 3 April 2013 / Revised: 15 May 2013 / Accepted: 20 May 2013 / Published: 24 May 2013
(This article belongs to the Special Issue Macrocyclic Chemistry)

Abstract

Macrocyclic scaffolds are commonly found in bioactive natural products and pharmaceutical molecules. So far, a large number of macrocyclic natural products have been isolated and synthesized. The construction of macrocycles is generally considered as a crucial and challenging step in the synthesis of macrocyclic natural products. Over the last several decades, numerous efforts have been undertaken toward the synthesis of complex naturally occurring macrocycles and great progresses have been made to advance the field of total synthesis. The commonly used synthetic methodologies toward macrocyclization include macrolactonization, macrolactamization, transition metal-catalyzed cross coupling, ring-closing metathesis, and click reaction, among others. Selected recent examples of macrocyclic synthesis of natural products and druglike macrocycles with significant biological relevance are highlighted in each class. The primary goal of this review is to summarize currently used macrocyclic drugs, highlight the therapeutic potential of this underexplored drug class and outline the general synthetic methodologies for the synthesis of macrocycles.
Keywords: macrocycles; macrocyclization; macrocyclic drugs; natural products; retrosynthesis; methodology; macrolactonization; macrolactamization; transition-metal catalyzed cross coupling; ring-closing metathesis; click chemistry macrocycles; macrocyclization; macrocyclic drugs; natural products; retrosynthesis; methodology; macrolactonization; macrolactamization; transition-metal catalyzed cross coupling; ring-closing metathesis; click chemistry
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Yu, X.; Sun, D. Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles. Molecules 2013, 18, 6230-6268.

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