Issue: #6February 2012
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Greetings!

 

NEW AT ADESIS

-Novel Imidazo[1,2-a] Pyridines by Adesis - Over 100 New Compositions of Matter Coming Soon.     

- 3 Easy Ways to Search the Adesis Catalog

- Visit Adesis at FLOHET 2012-Now Scheduling Meetings

- New Compounds for February -  Always In Stock!

 

 

In This Issue
Novel Imidazo [1,2-a] pyridines
3 Easy Ways to Search Our Online Catalog
FLOHET 2012
Compounds of the Month
February Promotion

 

catalog e-news

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THE NEW 2012 CATALOG

 

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Adesis Whitepaper

oct poster

Efficient Methods for Regioselective 

Functionalization of 

6-Substituted Furo[3,2-b] pyridines for Indole Isosteres.  

 

 

Quick Links

 


 

 

 

 

 


 

Novel Imidazo[1,2-a] Pyridines by Adesis -  Over 100 New Compositions of Matter Coming Soon 

  

By Andrew Cottone, VP of Chemistry

 

 

Imidazo[1,2-a] pyridines are a popular structural motif with therapeutic applications for antibacterial, antiviral and as inhibitors of phosphoinositide 3-kinase and angiogenesis.1,2,3,4  .  In a logical extension of the unique collection of the Adesis orthogonally substituted pyridines, we have introduced orthogonally-functionalized imidazo[1,2-a]pyridine building blocks (Table 1).

 

 

 



 

We have shown remarkable ability to control the substitution at positions 5,6,7, and 8 on this heterocycle.  With these advanced materials, differential reaction techniques (e.g.,  Metal-Halogen-Exchange or Pd cross coupling reactions) can be easily employed to quickly generate a series of qualified targets (Figure 1).

 

 

 


 

 

 

Adesis has also extended its Catalog to include electrophilic halogenations at the 3 position.  It can be further envisioned that differential reactivity of these positions will allow for inclusion of novel functional groups and efficient access to pharmaceutically relevant agents (Figure 2).

 

 


  

 

In conclusion, Adesis' program to design and synthesize novel imidazo[1,2-a]pyridines has also enabled scale-ups to multi-kilogram levels.  In our hands these compounds can be easily functionalized at each position for efficient generation of regio-isomers and advanced scaffolds.  In the near future Adesis will leverage its experience in heterocyclic chemistry to introduce well over 100 new compositions of matter in this family.

 

1)     Koubachi, J.; El Kazzouli, S.; Berteina-Raboin, S.; Mouaddib, A.; Guillaumet, G.; Journal of Organic Chemistry, 2007, 72, 7650-7655.

2)     Kim, O.; Jeoung, Y.; Lee, H.; Hong, S.; Hong, S. Journal of Medicinal Chemistry, 2011, 54, 2455-2466.

3)     Stec, M.; Andrews, K.; Booker, S.; Caenepeel, S.; Freeman, D.; Jinag, J.; Liao, H.; McCarter, J.; Mullady, E.; San Miguel, T.; Subramanian, R.; Tamayo, N.; Wang, L.; Yang, K.; Zalameda, L.; Zhang, N.; Hughes, P.; Norman, M.; Journal of Medicinal Chemistry, 2011, 54, 5174-5184.

4)     Enguehard, C.; Renou, J.; Collot, V.; Hervet, M.; Rault, S.; Gueiffer, A.; Journal of Organic Chemistry, 2000, 65, 6572-6575.


 

 

 

 

 

3 Easy Ways to Search Our Online Catalog 



 

 

 
FLOHET 2012
Florida Heterocyclic and Synthetic Conference

 

FlOHET Gainesville, Florida - March 4-7, 2012 

Come meet the Adesis CEO & CSO, Dr. Ving Lee  or schedule a meeting prior to the show Schedule Meeting

 
 

Compounds of the Month

Hot New Heterocycles 


We have recently introduced new Imidazo[1,2-a] pyridines into our catalog.  Below are the first examples to reach inventory.  Check back regularly as we expand the range of substitution.  Be sure to explore all our imidazo-pyridines and other novel heterocycles, too.  

 

 

 

To see all of our new heterocycles Click here 

 


 

 

About Adesis

Adesis, Inc. is a contract research organization (CRO) supporting the pharmaceutical and biopharmaceutical industry, biomaterials and catalysts industry. 

 

The life science industry has embraced the philosophy of outsourcing reference standards (competitor's drugs), targets, scaffolds, building blocks and advanced intermediates. Outsourcing allows medicinal chemists to focus on design and assembly of new targets for pharmacological evaluation and streamlines the early stage drug discovery process. Similarly, other chemistry-based research organizations (catalysts, biomaterials and fragrances) have accepted similar modus of operendi in order to maximize cost controls, while having timely project successes.

 

The core foundation of Adesis, Inc. is attributed to our experienced chemists with the expertise to conduct complex multi-step synthetic sequences (typical range of 2 - 20 steps).

 


 

15% Off Any 1 Gram Order

February Promotion: 

15% of any 1 gram catalog order.

 

Please call Jack Church to place your order: 302-323-6305 or email info@adesisinc.com

Offer Expires: March 15th 2012 
Only one offer per person 

We hope you have enjoyed reading our Adesis newsletter.  We welcome your comments.

 

With Best Wishes,

 

Paul Beard

  

If you are interested in how your company can do business with Adesis or to learn more about our capabilities, please contact one of the members of our business development team.

 

Ronald G. Yarger, PhD

Director, Business Development 

Ph. 302-261-3383; Mobile 302-358-8837 

E-mail: ryarger@adesisinc.com

 

Paul Beard, MBA BS 

Business Development Associate 

Ph. 302-323-6314; Mobile 302-383-5918                      

      E-mail: pbeard@adesisinc.com