| Original document(41 pages) 中文版 |
The present invention provides a method for producing an optically active 2-phenyl-2,3,-dihydroxypropyl azole derivative, which is a useful compound in the field of medicines and agricultural chemicals, and is, in particular, a significantly important intermediate in the step of producing an optically active azole antifungal agent. The present invention also provides new intermediates in the method. An optically active alpha -hydroxycarboxylic acid derivative represented by general formula (1) is used as a starting material and is allowed to react with an azole acetic acid derivative (2) to produce a new, optically active azole-alkyl ketone derivative (3). Subsequently, a new, optically active azole-methyl alcohol derivative (5) is produced by highly diastereoselective alkylation by an appropriate combination of a protective group and an organometallic reagent (4). Furthermore, the optically active azole-methyl alcohol derivative (5) is selectively deprotected to produce an optically active 2-phenyl-2,3-dihydroxypropyl azole derivative (6). The present invention provides a method for producing a new, optically active azole-alkyl ketone derivative, and a new, optically active azole-methyl alcohol derivative. According to the present invention, an optically active 2-phenyl-2,3-dihydroxypropyl azole derivative can be produced inexpensively and stably by simple steps. |
Application Number
申请号 |
03803736 |
Application Date
申请日 |
2003.02.07 |
| Title 名称 |
Optically active azole derivative and process for producing the same |
Publication Number
公开号 |
1630646 |
Publication Date
公开日 |
2005.06.22 |
| Approval Pub. Date |
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Granted Pub. Date |
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| International Classification 分类号 |
C07D249/08,C07D405/12,C07D401/06,C07D417/06 |
Applicant(s) Name
申请人 |
Mitsui Chemicals Inc. |
| Address 地址 |
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| Inventor(s) Name 发明人 |
Suzuki Tsuneji |
| Attorney & Agent 代理人 |
zhong jing |
| More information 更 多 信 息 |
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