| |
The objective of the technology is to develop proprietary technology for Aromatic C-N, C-C and Ar-Ar bond formation. C-N bonds program was developed based on Buchwald technology. The palladium-catalysed formation of aromatic carbon-hetero-atom bonds is increasingly becoming useful tool especially for those who are in the discovery labs of the pharma companies. However, the current methodology needs to be matured and perhaps more successful examples process research and scale up of the transformations from the lab to commercial is being carried out at Shasun.
Arylhydrazones were studied as an initial set of molecules under this study. Arylhydrazones will lead to indoles and there are many molecules, which has indole-based structures such as Sumatriptan, Zafirlukast, Indomethacin etc. The advantage of using Pd catalyzed methodology in lieu of the classical reactions of analines with diethanolamines include 1) no toxic intermediates, 2) a wide range of commercially available aryl halides as starting material, 3) no side reaction other than diarylation. Arylpiperazine structural motifs is common among pharmaceutical substances such as Aripiprazole, Ciprofloxacin etc.
Apart from Buchwald chemistry, under a corporate program in 2005, silane coupling for Aryl-Aryl bonds and C-C bonding using organo Znic chemistry was developed at Shasun Pharma solution at UK. A large toolbox of catalysts/lgands/solvents /base systems to rapidly satisfy the increasing customer needs for more convergent syntheses are now available. |
