Drug Discovery and Development

  • Home Drug Discovery and Development
  • Drug Discovery
  • Genomics/Proteomics
  • Oncology
  • Neurological Disease
  • Infectious Disease
  • R&D 100 Awards
  • Pharma 50
    • 2022 Pharma 50
    • 2021 Pharma 50

A New Method Cuts The Cost of Drug-Building Chemicals

By Ecole Polytechnique Federale de Lausanne | August 12, 2016

The amines are one of the most important classes of chemical compounds today. Amines that contain a ring-like structure – called an “aryl” group – are used widely in pharmaceuticals, such as the top-selling drugs Abilify, Crestor, Gleevec, and Lidoderm. EPFL scientists have now developed a method to produce aryl-containing amines in a cheap and easily scalable way. The work is published in Nature Communications.

Aromatic and heteroaromatic amines ((hetero)aryl amines) are central to medicinal chemistry. The process of making different amines is called amination, which involves connecting an amine to an organic molecule. The amine itself must first be prepared in advance by the hydrogenation of anilines, which are used as a nitrogen source and are derived from nitroarenes.

Xile Hu and Chi Wai Cheung at EPFL have now developed a new method for making (hetero)aryl amines through the reductive coupling of nitroarenes with organic compounds, without needing to go through the aniline step first. Using a simple iron catalyst, the researchers were able to couple amines to a number of alkyl halides, a group of organic compounds widely used in commercial products.

The method was shown to have a high tolerance to functional groups – including some that require protection under conventional amine synthesis – making them versatile and well suited for a broad range of applications.

The new method allows chemists to synthesize alkyl or aryl amines from directly from nitroarenes, which are often cheaper than anilines. Moreover, using nitroarenes directly is more step-economical than using anilines, since the latter have to be derived from nitroarenes anyway. In addition, certain anilines containing are difficult to produce, while their corresponding nitroarenes are readily available.

The authors state: “From these points of view, the current method can be considered as a valuable alternative to the conventional amination methods such as direct alkylation and reductive amination.”


Filed Under: Drug Discovery

 

Related Articles Read More >

Roche in Drug Discovery & Development Pharma 50
Roche’s bispecific antibody Lunsumio wins priority review from FDA for non-Hodgkin lymphoma
Tiffany Hurd
CB Therapeutics biz dev lead sees upside for psychedelics in mental health and beyond
Pharmacovigilance
A new era of pharmacovigilance: Worldwide master key for drug safety monitoring
Takeda Pharmaceutical in the Drug Discovery & Development Pharma 50
Takeda’s Takhzyro fares well in pediatric hereditary angioedema study

MEDTECH 100 INDEX

Medtech 100 logo
Market Summary > Current Price
The MedTech 100 is a financial index calculated using the BIG100 companies covered in Medical Design and Outsourcing.

Need Drug Discovery news in a minute?

We Deliver!
Drug Discovery & Development Enewsletters get you caught up on all the mission critical news you need. Sign up today.
Enews Signup
Drug Discovery and Development
  • MASSDEVICE
  • DEVICETALKS
  • Medical Design & Outsourcing
  • MEDICAL TUBING + EXTRUSION
  • MEDTECH 100
  • Medical Design Sourcing
  • Subscribe to our Free E-Newsletter
  • Contact Us
  • About Us
  • Advertise With Us
  • R&D World
  • Drug Delivery Business News
  • Pharmaceutical Processing World

Copyright © 2022 WTWH Media LLC. All Rights Reserved. The material on this site may not be reproduced, distributed, transmitted, cached or otherwise used, except with the prior written permission of WTWH Media
Privacy Policy | Advertising | About Us

Search Drug Discovery & Development

  • Home Drug Discovery and Development
  • Drug Discovery
  • Genomics/Proteomics
  • Oncology
  • Neurological Disease
  • Infectious Disease
  • R&D 100 Awards
  • Pharma 50
    • 2022 Pharma 50
    • 2021 Pharma 50