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Updated: Dec 9, 2025

Facile Preparation of 2Z,4E-Dienamides by the Olefination of Electron-deficient Alkenes with Allyl Acetate
Published on: June 21, 2017
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients
Christian Gampe1, Vishal A Verma1
1Genentech, 1 DNA Way, South San Francisco, 94080 California, United States.
Abstract:
There is a dichotomy between the increasing utility of aldehydes as tool molecules that bind to "undruggable" protein sites and the designation of the aldehyde functional group as a structural alert by the medicinal chemistry community. Herein we compile information about pharmacologically active aldehydes that are being used in humans. We summarize the learnings from these data, discuss advantages and challenges associated with aldehydes, and derive strategies for the successful development of aldehydes within drug discovery programs.
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