C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/476.3, 260/5
C07D 333/24 (2006.01) C07C 149/40 (1980.01)
Patent
CA 1103684
ABSTRACT OF THE DISCLOSURE Anti-inflammatory agents such as salicylic acid, pyra- zolone derivatives, indomethacin, etc. generally exhibit potent anti-inflammatory activity, but they also have serious side effects associated with them. The present invention provides a method of producing anti-inflammatory compounds not having as pronounced side effects. The compounds are 2-thio-2-substituted-alkanoic acid derivatives represented by the formula (I) Image (I) wherein A represents (1) a substituted-phenyl group of the formula Image in which y1 represents an isobutyl group or an unsubstituted- or substituted-phenoxy group wherein the substituent is a halogen atom, a trifluoromethyl group or an alkoxy group having 1 to 4 carbon atoms, or (2) a substituted-thienyl group of the formula Image in which y2 represents an alkyl group having 1 to 4 carbon atoms; R represents an alkyl group having 1 to 4 carbon atoms; R3 represents a phenyl group, an alkyl-phenyl group wherein the alkyl group has 1 to 4 carbon atoms, or an alkyl group having 1 to 4 carbon atoms; and R4 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms The process comprises reacting a 2-(arylthio or alkylthio)-2-substituted-acetic acid of the formula (III) Image (III) wherein A and R3 are as defined above, with an alkylating agent represented by the formula (II) RZ (II) wherein R is as defined above and Z represents a halogen atom , an alkyl- or arylsulfonyloxy group or a sulfuric acid ester residual group in the presence of at least 2 mols of a base per mole of the 2-(arylthio or alkylthio)-2-substituted-acetic acid, to form the compound of the formula (I) wherein R4 represents a hydrogen atom and, optionally, converting the resulting compound to the compound of the formula (I) wherein R4 represents an alkyl group by esterification.
309676
Kishi Kumiko
Kondo Kiyosi
Negishi Akira
Suda Minoru
Tunemoto Daiei
George H. Riches And Associates
Sagami Chemical Research Center
LandOfFree
Process for preparing 2-thio-2-substituted-alkanoic acid... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Process for preparing 2-thio-2-substituted-alkanoic acid..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process for preparing 2-thio-2-substituted-alkanoic acid... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-241039