Title:
SYNTHESIS OF ALPHA-SUBSTITUTED ACRYLIC ACID AND ITS APPLICATION
Document Type and Number:
Japanese Patent JP3845806
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To readily obtain the subject compound useful as a raw material, etc., for medicines in high yield from inexpensive raw materials by reacting a halide with a malonic ester, etc., saponifying the resultant alkyl malonate and then carrying out the Mannich reaction of the obtained compound with an organic base and formaldehyde.
SOLUTION: A compound represented by formula I [R1 is H, a (cyclo)alkyl, a (halogen-substituted)phenyl, CF3 or the like; R2 is H or R1; Y is a halogen; (n) is 0-10] is reacted with a compound represented by formula II (R8 is a 1-4C alkyl) in a solution of an alkali metal in an alcohol, etc., to provide a compound represented by formula III, which is subsequently saponified in the presence of an aqueous solution of a base to afford a diacid. The resultant diacid is then subjected to the Mannich reaction with an oreganic base and foramaldehyde to provide a compound represented by formula IV.
Inventors:
Pierre Duhamel
Rousset Duhamel
Duni Danvi
Thierry Monail
Jeanne-Marie Le Comte
Jean-Charles Schwartz
Rousset Duhamel
Duni Danvi
Thierry Monail
Jeanne-Marie Le Comte
Jean-Charles Schwartz
Application Number:
JP7317096A
Publication Date:
November 15, 2006
Filing Date:
March 04, 1996
Export Citation:
Assignee:
Societe Civil Bioproge
International Classes:
C07C57/04; B01J27/20; C07D317/60; C07B61/00; C07C51/09; C07C51/347; C07C51/353; C07C57/42; C07C57/54; C07C57/58; C07C59/42; C07C59/60; C07C67/343; C07C69/612; C07C201/12; C07C205/50; C07C227/02; C07C229/30; C07C229/34; C07C255/41; C07C319/18; C07C319/20; C07C323/50; C07C323/56; C07C327/32; C07D317/68; C07C323/27; C07C323/29; (IPC1-7): C07C57/04; B01J27/20; C07C51/09; C07C57/42; C07C57/54; C07C57/58; C07C59/42; C07C59/60; C07C69/612; C07C201/12; C07C205/50; C07C227/02; C07C229/30; C07C229/34; C07C255/41; C07C323/50; C07C323/56; C07C327/32; C07D317/60; //C07B61/00
Domestic Patent References:
| JP61165362A | ||||
| JP4501868A |
Foreign References:
| WO1993008162A1 |
Attorney, Agent or Firm:
Takashi Koshiba