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Introduction
In the field of pharmaceuticals, there is a constant demand for new and improved drugs to treat a variety of diseases.
One such drug that has garnered attention recently is (+)-3-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy, which is commonly referred to as UM764.
UM764 is a potent and selective G protein-coupled receptor kinase 2 (GRK2) inhibitor, which has shown promise in preclinical studies as a potential treatment for a range of diseases, including cancer, Parkinson's disease, and Alzheimer's disease.
One of the key challenges in the development of UM764 has been the synthesis of its active ingredient.
The natural product is derived from the bacterium Streptomyces hygroscopicus, and its total synthesis has proven to be quite challenging.
In order to overcome this hurdle, a number of synthetic routes to UM764 have been developed, each with its own advantages and challenges.
In this article, we will explore the synthetic routes that have been developed for the synthesis of UM764 and their applications in the chemical industry.
Synthetic Routes to UM764
There are several synthetic routes that have been developed for the synthesis of UM764.
One of the most widely used routes involves the synthesis of the key intermediate, N-[(1S)-1-(dibenzylamino)propyl]-3-carboxy-2,2,5,5-tetramethyl-1-oxy-pyrrolidine-2,5-dione (DIBAL-H), which is then hydrolyzed to form UM764.
This route is illustrated below:
Figure 1: Synthesis of UM764 via DIBAL-H intermediate
Another route involves the synthesis of UM764 directly from the naturally occurring intermediate, (1S)-1-(dibenzylamino)propyl alcohol (DBA) using a sequence of chemical reactions.
This route is shown below:
Figure 2: Synthesis of UM764 via DBA intermediate
Both of these routes have their own advantages and challenges.
The DIBAL-H route offers greater control over the synthesis and allows for the introduction of functional groups at specific positions, while the DBA route is more atom efficient and does not require the introduction of a protecting group.
Applications in the Chemical Industry
The development of synthetic routes to UM764 has important implications for the chemical industry, particularly in the pharmaceutical and agrochemical sectors.
UM764 and its derivatives hold great promise as potential drugs, and the ability to synthesize them in the laboratory will allow for their further study and development.
In addition, the development of synthetic routes to UM764 will enable the large-scale production of these compounds, which is essential for their use in drug development and commercialization.
Another important application of synthetic routes to UM764 is in the development of agrochemicals.
UM764 and its derivatives have been shown to have a range of biological activities, including herbicidal, insecticidal, and fungicidal activity, making them promising candidates for use in crop protection.
The ability to synthesize UM764 and its derivatives in the laboratory will enable their introduction into the agrochemical market, where they can be used to improve crop yields and protect against pests and diseases.
Conclusion
In conclusion, the development of synthetic routes to UM764 is a significant advancement in the field of chemical synthesis and has important implications for the pharmaceutical and agrochemical sectors.
The ability to synthesize UM764 and its derivatives in the laboratory will enable their further study and development as potential drugs and agrochemicals, and