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Tuesday 17 June 2014

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

 Graphical abstract: 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

*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

Monday 16 June 2014

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

 

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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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A TWO-STEP TANDEM REACTION TO PREPARE HYDROXAMIC ACIDS DIRECTLY FROM ALCOHOLS | ORGANIC CHEMISTRY SELECT

A TWO-STEP TANDEM REACTION TO PREPARE HYDROXAMIC ACIDS DIRECTLY FROM ALCOHOLS | ORGANIC CHEMISTRY SELECT:



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Wednesday 11 June 2014

Boronic Acid Catalyzed Annulation of a Pyran Ring



Boronic Acid Catalyzed Annulation of a Pyran Ring

A route to oxygenated pyrano[3,2-a]- and pyrano[2,3-a]carbazole alkaloids
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Amine Methylation Made Easy



Amine Methylation Made Easy

A mild and catalytic methylation of amines with formic acid
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