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Racemization refers to the phenomenon of eliminating the optical properties of chiral compounds, so that they no longer rotate light. Racemization can be achieved through two methods: racemization and internalization. Below, we will provide a detailed introduction to the differences between these two methods and their applications in drug synthesis

Racemization refers to the introduction of other chiral substances outside a compound, causing a chiral compound to combine with other chiral substances to form a mixture of optical enantiomers. Through appropriate experimental conditions, the optical properties of this optical mixture can be reduced or eliminated, achieving chiral racemization. The implementation of racemization requires the selection of chiral reagents that have specific interactions with the target compound. Common chiral reagents include asymmetric synthesis reagents, enzymes, and amino acids. The advantage of racemization is its wide application in drug synthesis, which can efficiently eliminate the optical rotation of chiral compounds, improve the pharmacokinetic properties of compounds, and enhance the therapeutic effect of drugs

Internal racemization refers to the process of achieving racemization within chiral compounds in a certain way. Unlike racemization, racemization does not require the introduction of other chiral reagents. Common racemization methods include physical and chemical methods. Physical methods mainly include crystal shape modification, suspension method, and concentration method, which achieve racemization by changing the physical properties of compounds. Chemical methods involve deactivating chiral centers through chemical reactions, thereby eliminating the chiral properties of compounds. The advantage of racemization is that it does not require the introduction of other chiral reagents, which is more simplified and economical, but its application range is relatively narrow

Racemization and internalization have wide applications in drug synthesis. Racemization is mainly used to eliminate the optical rotation of chiral compounds and plays a crucial role in synthesis and purification processes. For example, when synthesizing polar isomers with medicinal value, racemization can eliminate the optical rotation of two optical isomers, making the synthesized product meet market demand. In addition, racemization can also be used to synthesize chiral drugs with specific pharmacological effects. The application of racemization in drug synthesis is relatively limited, but it still has certain research value

Overall, racemization, as an important chiral control method, has significant theoretical and practical value. Through racemization and internalization, we can effectively change the optical rotation characteristics of chiral compounds, thereby improving the performance of drugs or synthesizing specific chiral drugs. In the future, with the continuous development of technology, racemization methods will be further improved and innovated, providing more solutions for drug synthesis and chiral processes.