Synthetic Approaches Used in the Scale‐Up of Macrocyclic Clinical Candidates

Kong, Jongrock

doi:10.1002/9781119092599.ch15

Cited by 1 publication

(2 citation statements)

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“…4 In 2015 Kong published a review on the synthesis of macrocyclic clinical candidates that included a section on ring-closing metathesis (RCM) and presented a nice comparison of macrocyclization approaches. 5 In 2016 Fogg and co-workers reviewed pharmaceutical and fine chemical applications of the metathesis reaction, including a discussion of simeprevir, the first approved drug that includes a metathesis reaction in its manufacturing route, promoted by M2 catalyst 4. 6 The current article, a follow up to a previous review on the metathesis reaction that covered the patent literature up to year 2015, 7 is focused on pharmaceutical applications published in the patent literature during the years 2016 and 2017.…”

Section: Introductionmentioning

confidence: 99%

“…The development of the RCM for ciluprevir and other HCV drug candidates was further reviewed by the Boehringer-Ingelheim team in 2014 and well as Farina and Horvath in a 2015 review chapter . In 2015 Kong published a review on the synthesis of macrocyclic clinical candidates that included a section on ring-closing metathesis (RCM) and presented a nice comparison of macrocyclization approaches . In 2016 Fogg and co-workers reviewed pharmaceutical and fine chemical applications of the metathesis reaction, including a discussion of simeprevir, the first approved drug that includes a metathesis reaction in its manufacturing route, promoted by M2 catalyst 4 …”

Section: Introductionmentioning

confidence: 99%

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Olefin Metathesis in Drug Discovery and Development—Examples from Recent Patent Literature

Hughes

Wheeler

Ene

2017

Org. Process Res. Dev.

108

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The olefin metathesis reaction is finding increasing use in drug discovery and process chemistry, with a number of applications now implemented at commercial manufacturing scale. Catalyst improvements over the past decade have allowed use of the metathesis reaction with highly functionalized substrates, allowing chemists to access increasingly diverse chemical space, including most notably macrocycles, constrained small ring spirocycles, and fused-ring systems. For scientists employed in the pharmaceutical industry, the patent literature is the primary avenue for communication of synthetic routes to drug candidates. While most examples of the metathesis reaction in the patent literature offer only sketchy experimental details and provide little context on reaction development, the wide scope of substrates within the pharmaceutical patent literature provides a true indication of reaction scope and functional group compatibility. The current article reviews applications of the metathesis reactions in drug discovery and development in the pharmaceutical industry disclosed in the patent literature from January 2016 to August 2017.

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