OPTICALLY ACTIVE AZOLE DERIVATIVE AND METHOD FOR PRODUCING THE SAME

• Main Authors: SUZUKI TSUNESHI, TSUNODA HIDETOSHI
• Format: Patent
• Language: English
• Published: 30.04.2004
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

PROBLEM TO BE SOLVED: To provide a method for stably producing an optically active 2-phenyl-2,3-dihydroxypropylazole derivative useful in pharmaceutical and agrochemical field and an extremely important intermediate in the production of an optically active azole antimycotic agent in a short step at a low cost and provide a new intermediate. SOLUTION: A new optically active azole alkyl ketone derivative (3) is produced by using an optically active α-hydroxycarboxylic acid derivative expressed by general formula (1) as a starting raw material and reacting the material with an azoleacetic acid derivative (2). A new optically active azole methyl alcohol derivative (5) is produced by a highly diastereo-selective alkylation reaction by a combination of a protective group and an organometallic reagent (4). Furthermore, an optically active 2-phenyl-2,3-dihydroxypropylazole derivative (6) is produced by the selective deprotection of the derivative (5). The structure formula and reaction formula are shown below. COPYRIGHT: (C)2004,JPO