- Pd/PTABS: Low-Temperature Thioetherification of Chloro(hetero)arenes
-
The thioetherification of heteroaryl chlorides is an essential synthetic methodology that provides access to bioactive drugs and agrochemicals. Due to their (actual or potential) industrial importance, the development of efficient and low-temperature protocols for accessing these compounds is a requirement for economic and ecologic reasons. A particular highly effective catalytic protocol using the Pd/PTABS system at only 50 °C was developed accordingly. The coupling between chloroheteroarenes and a variety of less reactive arylthiols and alkylthiols was carried out with a high efficiency. Heteroarenes of commercial relevance such as purines and pyrimidines were also found to be useful substrates for the reported transformation. The commercial drug Imuran (azathioprine) was synthesized as an example, and its preparation could be optimized. DFT studies were performed to understand the electronic effects of the tested ligands on the catalytic reaction.
- Bandaru, Siva Sankar Murthy,Bhilare, Shatrughn,Cardozo, Jesvita,Chrysochos, Nicolas,Schulzke, Carola,Sanghvi, Yogesh S.,Gunturu, Krishna Chaitanya,Kapdi, Anant R.
-
p. 8921 - 8940
(2019/07/08)
-
- Concatamers for Immunemodulation
-
The invention relates to a polymeric, non-coding nucleic acid molecule for modulation of the activity of the human and animal immune system as well as a method for the manufacture thereof and a vaccine, comprising the polymeric, non-coding nucleic acid molecule, wherein polymeric, non-coding nucleic acid molecules may be understood as non-coding nucleic acid molecules, comprising at least four covalently bound molecules (tetramer) or are assemblies of more non-coding nucleic acid molecules (high molecular polymers) which are covalently bound to each other.
- -
-
-
- Chemical transformations of 6-[(1-methyl-4-nitro-5-imidazolyl)-thio]purine (azathioprine)
-
The chemical transformations of 6-[(1-methyl-4-nitro-5-imidazolyl)thio]purine (azathiopurine)- hydrogenation, acetylation, alkylation by lower alkyl halides at positions 7 and 9 of the purine ring, hydrolytic cleavage at the C(6)-S and S-C(5) bonds - were studied.
- Kochergin,Aleksandrova,Korsunskii
-
p. 311 - 318
(2007/10/03)
-
