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Hydrazino-Spengler Essay

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8. Hydrazino-Pictet-Spengler ligation reaction = In this reaction, the aliphatic and aromatic hydrazines are used as a substrate to undergo pictet-spengler reaction with aldehydic and ketonic group. As described in the above category 7, the various substrates are used for ligation with aldehydic and ketonic groups of the proteins, P. Agarwal and research group developed the Hydrazino-Pictet-Spengler(HIPS) ligation reaction so that the stable protein conjugates can be developed . This strategy can be used in the development of a prodrug delivery system. The advantage of this scheme over the other oxime and hydrazone ligations is that the ligation proceeds very fast near the neutral pH(that is the pH of the normal physiological body) and the product of the HIPS ligation is showing very long stability in human plasma (approx 5 days) as compared to that of oxime-linked conjugate (approx 1 day). This was monitered by protein-fluorophore conjugates by ELISA(42). Scheme 18. Overview of the Hydrazino-Pictet-Spengler reaction. A) In reaction with a small molecule and B) protein aldehydes, a C−C bond (highlighted in red) is formed between the indole and the aldehyde of interest …show more content…

It is a very important reaction for the synthesis of the larged fused heterocyclic compounds. Researchers have developed a lot of series of fused heterocycles and analyzed them for their physiological and therapeutic effect. Many new drugs are there in the market that are being synthesised from this valuable and novel reaction. The researchers have also undergone experiments regarding the effect of using various types of substrates, solvent system, catalyts, temperature and many other parameters on the rate and yield of the reaction. Still a lot of research work is being going on to bring the modifications in the reations. In short, this reaction has a bright future aspects in terms of research

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