Title:
REAGENT FOR STEREOSPECIFIC FLUOROMETHYLATION AND PROCESS THEREFOR
Document Type and Number:
Japanese Patent JP3157180
Kind Code:
B2
Abstract:
PURPOSE: To provide the subject reagent which consists of specific magnesium benzyl fluoromalonate, allows the introduction of fluoromethyl group into the carbon of a carbonyl group and yields fluoromethyl ketone at a high yield by reacting with an imidazolide of a carboxylic acid.
CONSTITUTION: The objective stereospecific fluoromethylation reagent which is expressed by formula II and allows the introduction of the fluoromethyl group into the carbon of the carbonyl in an org. structural body is obtd. by bringing the dimethyl ester of fluoromalonic acid expressed by formula I into transesterification reaction at 50 to 100°C with a compd. (e.g. benzyl alcohol, etc.) of formula; R'XH (R' is a group cleavable by hydrogen cracking of an aralkyl, etc.; X is S, O) in the presence of a strong acid catalyst, removing the formed methanol by distillation under a reduced pressure, then hydrolyzing only one of the two ester groups by using an alkali metal hydroxide in a lower aliphat. alcohol (e.g. isopropanol, etc.) and bringing a magnesium alkoxide into reaction therewith.
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Inventors:
James T. Palmer
Application Number:
JP4417291A
Publication Date:
April 16, 2001
Filing Date:
February 15, 1991
Export Citation:
Assignee:
Prototech, Inc.
International Classes:
C07B41/12; C07B45/00; C07B61/00; C07C45/41; C07C45/67; C07C49/753; C07C67/10; B01J23/40; C07C67/343; C07C69/63; C07C69/716; C07C69/738; C07C205/43; C07C221/00; C07C225/06; C07C227/02; C07C229/22; C07C271/18; C07C271/20; C07C271/22; C07C279/14; C07C303/26; C07C327/22; C07D207/08; C07D207/273; C07D307/33; C07C309/73; C07D207/26; (IPC1-7): C07C69/63; C07C45/41; C07C49/753; C07C221/00; C07C225/06; C07C227/02; C07C229/22
Domestic Patent References:
| JP6034938A | ||||
| JP55145647A |
Other References:
Ａｎｇｅｗ．Ｃｈｅｍ．Ｉｎｔ．Ｅｄ．Ｅｎｇｌ．，１９７９，Ｖｏｌ．１８，Ｎｏ．１，ｐ．７２−７４
Attorney, Agent or Firm:
Shusaku Yamamoto