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Document Type and Number:
WIPO Patent Application WO/2016/167225
Kind Code:
The purpose of the present invention is to provide a method for producing 2-halogenated benzoic acids, the method imparting high regioselectivity (high selectivity) and having a shorter reaction time than does the conventional reaction. This method for producing 2-halogenated benzoic acids, in order to achieve the above purpose, is characterized in that benzoic acids and a halogenating agent are reacted in the presence of an alkaline compound, making it possible to highly selectively obtain 2-halogenated benzoic acids.

TAKANO, Katsumi (346-1, Miyanishi, Harima-cho, Kako-gu, Hyogo 45, 〒6750145, JP)
FUJIWARA, Takeshi (346-1, Miyanishi, Harima-cho, Kako-gu, Hyogo 45, 〒6750145, JP)
SHIRAISHI, Hiroyuki (346-1, Miyanishi, Harima-cho, Kako-gu, Hyogo 45, 〒6750145, JP)
MATSUO, Nami (346-1, Miyanishi, Harima-cho, Kako-gu, Hyogo 45, 〒6750145, JP)
Application Number:
Publication Date:
October 20, 2016
Filing Date:
April 11, 2016
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SUMITOMO SEIKA CHEMICALS CO., LTD. (346-1, Miyanishi Harima-cho, Kako-gu, Hyogo 45, 〒6750145, JP)
ZERIA PHARMACEUTICAL CO., LTD. (10-11, Nihonbashi Kobuna-cho Chuo-k, Tokyo 51, 〒1038351, JP)
International Classes:
C07C51/363; C07C65/21
Domestic Patent References:
Foreign References:
Other References:
AUERBACH, JOSEPH ET AL.: "N-Bromosuccinimide/ dibromodimethylhydantoin in aqueous base: a practical method for the bromination of activated benzoic acids", TETRAHEDRON LETTERS, vol. 34, no. 6, 1993, pages 931 - 934, XP003002198, ISSN: 0040-4039
ALAM, ASHRAFUL ET AL.: "Total synthesis of 3,3',4-tri-O-methylellagic acid from gallic acid", TETRAHEDRON, vol. 63, no. 42, 2007, pages 10454 - 10465, XP022230666, ISSN: 0040-4020
HARAYAMA, TAKASHI ET AL.: "Concise synthesis of fagaridine and decarine, phenolic benzo[c]phenanthridine alkaloids, using the palladium-assisted biaryl coupling reaction", HETEROCYCLES, vol. 59, no. 1, 2003, pages 293 - 301, XP003002199, ISSN: 0385-5414
NGUYEN, THI-HUU ET AL.: "First General, Direct, and Regioselective Synthesis of Substituted Methoxybenzoic Acids by Ortho Metalation", JOURNAL OF ORGANIC CHEMISTRY, vol. 72, no. 9, 2007, pages 3419 - 3429, XP055321842, ISSN: 0022-3263
See also references of EP 3284734A4
Attorney, Agent or Firm:
SAMEJIMA, Mutsumi et al. (AOYAMA & PARTNERS, Umeda Hankyu Bldg. Office Tower 8-1, Kakuda-cho, Kita-ku, Osaka-sh, Osaka 17, 〒5300017, JP)
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