Title:
METHOD FOR SYNTHESIS OF (3-FLUOROOXETAN-3-YL)METHYL 4-METHYLBENZENESULFONATE
Document Type and Number:
WIPO Patent Application WO/2023/000636
Kind Code:
A1
Abstract:
A method for synthesis of (3-fluorooxetan-3-yl)methyl 4-methylbenzenesulfonate. A target product is prepared by using diethyl 2-fluoromalonate as a raw material and by means of a methylolation reaction, a hydroxyl protection reaction, a reduction reaction, an esterification reaction, a deprotection reaction, and a ring closure reaction in six steps. The steps are simple, the operation is easy, the raw material utilization rate and the product yield are high, intermediates are easy to separate, and the method is suitable for industrial scale-up production in terms of process safety, cost, raw material utilization rate, product purity, and the like. The results of embodiments show that the total yield of the reactions in the six steps of the method is 40-60%, and the HPLC purity of the target product (3-fluorooxetan-3-yl)methyl 4-methylbenzenesulfonate is greater than 97%.
Inventors:
LIU YANG (CN)
WEI YUANBO (CN)
WANG QIUFENG (CN)
XUE DUOQING (CN)
WU YONG (CN)
WEI YUANBO (CN)
WANG QIUFENG (CN)
XUE DUOQING (CN)
WU YONG (CN)
Application Number:
PCT/CN2022/073363
Publication Date:
January 26, 2023
Filing Date:
January 24, 2022
Export Citation:
Assignee:
ACCELA CHEMBIO CO LTD (CN)
International Classes:
C07D305/08
Domestic Patent References:
| WO2016184313A1 | 2016-11-24 |
Foreign References:
| US20170107190A1 | 2017-04-20 | |||
| CN107793381A | 2018-03-13 | |||
| CN113461643A | 2021-10-01 |
Other References:
BOYD SCOTT; DAVIES CHRISTOPHER D.: "A new and versatile synthesis of 3-substituted oxetan-3-yl methyl alcohols", TETRAHEDRON LETTERS, ELSEVIER, AMSTERDAM , NL, vol. 55, no. 30, 1 January 1900 (1900-01-01), Amsterdam , NL , pages 4117 - 4119, XP028861813, ISSN: 0040-4039, DOI: 10.1016/j.tetlet.2014.06.024
Attorney, Agent or Firm:
BEIJING FINELAND IP FIRM (CN)
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