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Racemization refers to a phenomenon in which an optical property in a compound having chirality is eliminated so that it no longer rotates light. Racemization can be achieved in two ways: racemization and meso-racemization. Below we will detail the differences between these two methods and their application in drug synthesis.
racemization refers to the introduction of other chiral substances outside the compound, so that the compound with chirality is combined with other chiral substances to form a mixture of optical enantiomers. Through the appropriate experimental conditions, the optical properties of the optical mixture can be reduced or disappeared, and the racemization of the chiral can be achieved. The realization of racemization requires the selection of chiral reagents that specifically interact with the target compound, and common chiral reagents include asymmetric synthesis reagents, enzymes and amino acids. The advantage of racemization is that it has a wide range of applications in drug synthesis, can efficiently eliminate the optical rotation of chiral compounds, and can also improve the pharmacokinetic properties of compounds and improve the efficacy of drugs.
mesogenic means that racemization is achieved by some means within a compound having chirality. Unlike racemization, meso-racemization does not require the introduction of other chiral reagents. Common ways of meso-racemization include physical and chemical methods. Physical methods mainly include crystal shape change method, suspension method and concentration method, which realize racemization by changing the physical properties of compounds. The chemical method is to inactivate the chiral center by chemical reaction and eliminate the chiral nature of the compound. The advantage of meso is that it does not need to introduce other chiral reagents, which is more simplified and economical, but the application range is relatively narrow.
racemization and meso-racemization have a wide range of applications in drug synthesis. Racemization is mainly used to eliminate the optical rotation of chiral compounds and plays a key role in the synthesis and purification process. For example, when a polar hetero preparation with medicinal value is synthesized, racemization can eliminate the optical rotation of the two optical isomers, so that the synthesized product meets the market demand. In addition, racemization can also be used for the synthesis of chiral drugs with specific pharmacological effects. The application of mesocization in drug synthesis is relatively small, but it still has some research value.
In general, as an important means of chiral control, racemization has important theoretical and practical value. Through racemization and meso-racemization, we can effectively change the optical properties of chiral compounds, and then improve the performance of drugs or synthesize drugs with specific chirality. In the future, with the continuous development of technology, racemization methods will be more improved and innovative, providing more solutions for drug synthesis and chiral processes.
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