ChemicalBook CAS DataBase List (1R,2R)-2-(3,4-difluorophenyl)cyclopropanecarboxylic acid

(1R,2R)-2-(3,4-difluorophenyl)cyclopropanecarboxylic acid synthesis

10synthesis methods

Product Name:(1R,2R)-2-(3,4-difluorophenyl)cyclopropanecarboxylic acid
CAS Number:220352-36-3
Molecular formula:C10H8F2O2
Molecular Weight:198.17

867-13-0
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1006376-60-8 Synthesis

(1S)-2-chloro-1-(3,4-difluorophenyl)-1-ethanol

1006376-60-8
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(1R,2R)-2-(3,4-difluorophenyl)cyclopropanecarboxylic acid

220352-36-3
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Yield:220352-36-3 87%

Reaction Conditions:

with potassium tert-butylate in toluene at 30 - 50; for 30 h;Temperature;

Steps:

6 Example 6: Specific preparation of the compound of formula VII (1R, 2R) -2- (3,4-difluorophenyl) cyclopropanoic acid
Potassium tert-butoxide (4.3 g, 64 mmol) was added 40 ml of toluene, A solution of the compound of formula VIII, phosphonoethyl triethyl ester (11.4 g, 51.2 mmol) was added dropwise at a temperature of 30 ° C, Drop finished, A solution of the compound of formula IV (S) -2-chloro-1- (3,4-difluorophenyl) ethanol (2.46 g, 12.8 mmol) in 12 ml of toluene was added dropwise, Insulation 40 ~ 50 reaction 30 hours, Add 20 ml of water, Divide the water phase. Add 5 ml of toluene, 6 ml of methanol, 5 ml of 30% sodium hydroxide solution, 65 ° C for 1.5 hours. Spin the solvent, Add 20 ml of water, Toluene 20 ml, extraction, Points to oil phase, Water with concentrated hydrochloric acid to adjust the pH value of 2 to 3, Plus toluene 20 ml extraction, Oil phase dry, Spin dry 2.22 g of the compound of formula VII, Quickly after curing. Yield 87%.

References:

Shangyu Jing Xin Pharmaceutical Co., Ltd.;Shanghai Jingxin Bio-pharmaceutical Co., Ltd.;Huang Yue;Xu Miaohuan CN104744266, 2017, B Location in patent:Paragraph 0066; 0067; 0068; 0069; 0070; 0071; 0072-0081

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