PREPARATION METHOD OF 1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL)-CYCLOPROPANECARBOXYLIC ACID AND INTERMEDIATE OF THE SAME

WIPO Patent Application WO/2017/133424

A1

The present invention relates to a preparation method of 1-(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-cyclopropanecarboxylic acid, wherein 2-(2-thiobenzo[D][1,3]dioxol-5-yl) acetonitrile is used as an intermediate, firstly the intermediate is reacted with a bromination agent, an organic base hydrofluoride salt to generate 2-(2,2-difluorobenzo[D][1,3]dioxol-5-yl) acetonitrile, and then an annulation reaction and a hydrolysis reaction of the 2-(2,2-difluorobenzo[D][1,3]dioxol-5-yl) acetonitrile is successively performed to prepare the target product. Compared to existing technologies, the process of the present invention not only has increased yield, lower cost, and wide sources of raw materials, but also does not use hazardous material, has better safety standards and is suitable for industrialized production.

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TIAN GUANGHUI (CN)
CAO BIAO (CN)
WU JIANZHONG (CN)

PCT/CN2017/071135

August 10, 2017

January 13, 2017

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VIGONVITA LIFE SCIENCES SUZHOU CO LTD (CN)

C07D317/60

CN101910134A

2010-12-08

HAGOOLY, Y. ET AL.: "Synthesis of Difluoroaryldioxoles Using BrF3", ORGANIC & BIOMOLECULAR CHEMISTRY, vol. 9, no. 3, 30 December 2011 (2011-12-30), pages 902 - 905, XP055406727
KUROBOSHI, M. ET AL.: "A Facile Synthesis of alpha , alpha-difluoroalkyl Ethers and Carbonyl Fluoride Acetals by Oxidative Desulfurization-Fluorination", SYNLETT, vol. 4, 30 April 1994 (1994-04-30), pages 251 - 252

SUZHOU CREATOR PATENT & TRADEMARK AGENCY LTD. (CN)

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