Pharmaceutical intermediate - hydroxypropyl betaclodextrin

Propyl betaclodextrin is an ether derivative of betaclodextrin.The introduction of hydroxypropyl group opened the hydrogen bonds within the betacyclodextrin molecule, forming an amorphous mixture, greatly improving the water solubility, proving high safety, and even being used for intravenous injection.Therefore, it is considered as a potential substitute for maternal cyclodextrin.Betacyclodextrin reacts with epoxypropane under alkaline conditions. Under the catalysis of base, betacyclodextrin alkoxy anions attack the carbon atoms with the least substituents on the oxygen ring, where the steric hindrance is the least.Cyclodextrin and epoxypropane react easily to form 6 substituents in strong alkaline environment, and 2 substituents in weak alkaline condition.The hydroxyl groups at the 2, 3 and 6 sites are activated under strong alkaline conditions, and the steric resistance at the 6 sites is the least, and the substituents are easy to enter.Under the condition of weak alkalinity, the hydroxyl group in the 2 position is the most acidic and easy to be activated, so the 2 position is the main substitute.Cyclodextrins and their derivatives have long been thought to have rigid structures, an assumption that does not accord with their ability to form complex structures easily.The structure of cyclodextrins is relatively flexible. Experiments show that cyclodextrins are flexible not only in solution, but also in solid state through non-covalent bonding.The introduction of hydroxypropyl group opened the internal hydrogen bond of betacyclodextrin, making the framework flexible and the substituents have some room to move.This relatively flexible structure can better explain the improvement of its complex formation ability and its complex reaction kinetics.At present, shandong binzhou zhiyuan biotechnology co., ltd. is the largest manufacturer of cyclodextrin derivatives in China. The product quality is first-class in China and the product types are the most in the same industry.