Altering physical properties of pharmaceutical co-crystals in a systematic manner

 

 

Altering physical properties of pharmaceutical co-crystals in a systematic manner

Christer B. Aakeröy, Safiyyah Forbes and John Desper

CrystEngComm, 2014, 16, 5870 DOI:10.1039/C4CE00206G

 

Systematic structure–property studies on a series of co-crystals of potential cancer drugs with aliphatic dicarboxylic acids were undertaken. This study reveals that systematic changes to the molecular nature of the co-crystallizing agent combined with control over the way individual building blocks are organized within the crystalline lattice makes it possible to establish predictable links between molecular structure and macroscopic physical properties, such as melting behaviour and aqueous solubility. However, it is not possible to find any notable correlation between physical properties and chemical compositions in the absence of structural consistency.

Paper

Altering physical properties of pharmaceutical co-crystals in a systematic manner

Christer B. Aakeröy,*^a   Safiyyah Forbes^a and   John Desper^a  

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*Corresponding authors

^aDepartment of Chemistry, Kansas State University, 213 CBC Building, Manhattan, USA
E-mail: aakeroy@ksu.edu;
Fax: +1 785 532 6666 ;
Tel: +1 785 532 6096

CrystEngComm, 2014,16, 5870-5877

DOI: 10.1039/C4CE00206G

C–C Coupling Repertoire Grows ... Organic Synthesis: Reaction eases addition of chiral carbon centers to aryl groups

 

REVIVAL

This new reaction combines chiral secondary and tertiary boronic esters (left) with lithiated aryls to form intermediates that rearrange upon electrophile addition, yielding aryl-alkyl coupling products.

The revival of a nearly 50-year-old technique for forming carbon-carbon bonds may help ease the synthesis of aryl derivatives, such as drug candidates.

Varinder K. Aggarwal and coworkers at the University of Bristol, in England, have taken a venerable but neglected synthesis called Zweifel olefination and made it new again (Nat. Chem. 2014, DOI: 10.1038/nchem.1971).

C–C Coupling Repertoire Grows

Organic Synthesis: Reaction eases addition of chiral carbon centers to aryl groups

 http://cen.acs.org/articles/92/i24/CC-Coupling-Repertoire-Grows.html
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http://cen.acs.org/articles/92/i24/CC-Coupling-Repertoire-Grows.html


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