Abstract: The present invention relates to a process for the efficient preparation of highly optical pure chiral carvedilol. According to the present invention, a chiral oxazolidin-2-one or oxazolidin-2-thione having formula 2, produced from the reaction of N-protected 2-(2-methoxyphenoxy)ethylamine with a chiral glycidol derivative is used as a key intermediate for the preparation of the chiral carvedilol. Specifically, the process for the preparation of the chiral carvedilol comprises a) reacting a compound of formula 2 with a halogenation agent, a sulfonation agent or a mitsunobu reagent to activate a hydroxyl group of the compound of formula 2, followed by nucleophilic substitution reaction with 9H-4-hydroxy carbazole to produce a compound of formula 7, and b) subjecting the obtained compound of formula 7 to a deprotection reaction in a presence of an inorganic base to produce the targeted chiral carvedilol. The process of the present invention can be accomplished in a mild condition.

Abstract: There is provided a process for preparing a glycidyl derivative from 3-chloro-1,2-propanediol, comprising i) adding a phosphate salt to a solution into which 3-chloro-1,2-propanediol is dissolved into a solvent to produce glycidol, and ii) adding to the solution of step i) a base capable of releasing a glycidyl group from the glycidol and a substrate susceptible to nucleophilic attack to produce the desired glycidyl derivative by nucleophilic attack of the glycidyl group to the substrate.

Abstract: A process for the preparation of chiral 4-hydroxy-2-oxo-1-pyrrolidine acetamide includes adding sodium cyanide together with citric acid to a solution of chiral epichlorohydrin to obtain chiral 3-chloro-2-hydroxypropionitrile by ring opening reaction of the chiral epichlorohydrin, reacting the obtained product with an alcohol containing hydrochloride gas to obtain chiral 4-chloro-3-hydroxybutyric acid ester, and reacting the obtained product in a presence of a base with glycinamide or with glycine ester accompanied by ammonolysis with ammonia to produce the targeted chiral 4-hydroxy-2-oxo-1-pyrrolidine acetamide.