4 Process for the Resolution of Racemic Alcohol Compounds Containing Quaternary Chiral Carbon and Synthesis of Systhane Derivatives

摘要

The present invention provides a racemate of a quaternary asymmetric carbon-containing alcohol compound suitably designed as an intermediate of formula (1) in the asymmetric synthesis of cystane, an excellent azole compound as a fungicide, in the presence of acyljuge in an organic solvent at 0 to 60 ° C. Splitting into optically pure respective R- and S-isomers via transesterification with lipase or hydrolysis of esters of the alcohols at a temperature of and synthesis of cystane and its derivatives from each split isomer It is about.;Formula 1;Wherein X represents hydrogen or halogen, n represents the number of carbons. In the present invention, X represents the number of carbons having a hydroxy group and a compound substituted with chlorine at the carbon-4 position of hydrogen or benzene ring 1, 2, 3 , 4 was synthesized. Synthesized racemic alcohols using a lipase, the compound of n = 1 was completely divided to synthesize the azole compound of the target compound. In order to measure the cognition ability of the used lipases of the quaternary asymmetric carbon, n was increased and synthesized to perform transesterification reaction. In order to improve the cleavage, the cleavage was improved by selecting amines as a reagent to remove aldehydes generated during the reaction.