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(1R,2S)-Fluorocyclopropylamine tosylate

CAS No.
143062-84-4
Chemical Name:
(1R,2S)-Fluorocyclopropylamine tosylate
Synonyms
(1R,2S)-2-fluorocyclopropan-1-amine;Compound FL0046;Sitafloxacin Impurity 60;Sitafloxacin Impurity 51;Sitafloxacin Impurity 3 Tosic acid;[(1R,2S)-2-fluorocyclopropyl]azanium;(1R,2S)-Fluorocyclopropylamine tosylate;(1R,2S)-2-Fluorocyclopropylamine tosylate;(1R,2S)-2-Fluorocyclopropan-1-aMine tosylate;(1R,2S)-2-fluorocyclopropan-1-amine tosylic acid
CBNumber:
CB1360587
Molecular Formula:
C10H14FNO3S
Molecular Weight:
247.28
MDL Number:
MFCD01861147
MOL File:
143062-84-4.mol
MSDS File:
SDS
Last updated:2026-09-12 18:49:12

(1R,2S)-Fluorocyclopropylamine tosylate Properties

storage temp. Inert atmosphere,Room Temperature
Appearance White to off-white Solid
InChI InChI=1/C7H8O3S.C3H6FN/c1-6-2-4-7(5-3-6)11(8,9)10;4-2-1-3(2)5/h2-5H,1H3,(H,8,9,10);2-3H,1,5H2/t;2-,3+/s3
InChIKey XUWZMHVPMZXIRU-SKBSZHOONA-N
SMILES S(C1C=CC(C)=CC=1)(O)(=O)=O.F[C@H]1C[C@H]1N |&1:12,14,r|
CAS DataBase Reference 143062-84-4

SAFETY

Risk and Safety Statements

Symbol(GHS)  Exclamation Mark (GHS07)
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H332-H335
Precautionary statements  P261-P280-P305+P351+P338
HS Code  2921309990

(1R,2S)-Fluorocyclopropylamine tosylate price More Price(55)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Apolloscientific PC49351 (1R,2S)-2-Fluorocyclopropan-1-amine toluene-4-sulphonate 97% 143062-84-4 250mg $21 2026-06-04 Buy
Apolloscientific PC49351 (1R,2S)-2-Fluorocyclopropan-1-amine toluene-4-sulphonate 97% 143062-84-4 1g $24 2026-06-04 Buy
Apolloscientific PC49351 (1R,2S)-2-Fluorocyclopropan-1-amine toluene-4-sulphonate 97% 143062-84-4 5g $51 2026-06-04 Buy
Apolloscientific PC49351 (1R,2S)-2-Fluorocyclopropan-1-amine toluene-4-sulphonate 97% 143062-84-4 10g $98 2026-06-04 Buy
Apolloscientific PC49351 (1R,2S)-2-Fluorocyclopropan-1-amine toluene-4-sulphonate 97% 143062-84-4 25g $226 2026-06-04 Buy
Product number Packaging Price Buy
PC49351 250mg $21 Buy
PC49351 1g $24 Buy
PC49351 5g $51 Buy
PC49351 10g $98 Buy
PC49351 25g $226 Buy

(1R,2S)-Fluorocyclopropylamine tosylate Chemical Properties,Uses,Production

Application

(1R,2S)-2-fluorocyclopropylamine p-toluenesulfonate is an organic synthesis intermediate and a pharmaceutical intermediate that can be used in laboratory research and development processes as well as in chemical and pharmaceutical synthesis processes.

Synthesis

1,1,2-Tribromo-2-fluoroethane

598-67-4

p-Toluenesulfonic acid

104-15-4

Dimethyl malonate

108-59-8

(1R,2S)-FLUOROCYCLOPROPYLAMINE TOSYLATE

143062-84-4

(1) 1.32 kg of dimethyl malonate and 3.7 kg of 1,1,2-tribromo-2-fluoroethane were added to a 50 L three-necked flask and dissolved in 15 L of anhydrous dimethylformamide. The flask was placed in a 25 °C water bath and 4.4 kg of anhydrous potassium carbonate was added in batches under stirring for 60 hours. After completion of the reaction, 30 L of ice water was added, extracted with ethyl acetate (8 L x 5), the organic phases were combined, washed to neutrality with saturated aqueous sodium chloride, dried over anhydrous sodium sulfate, and the solvent was evaporated. The residue was added to 3 L of ether and stirred in an ice bath for 4 h. It was filtered to yield 1.7 kg of solid A. (2) Solid A was added to a 10 L hydrogenation autoclave, dissolved with 6 L of methanol, and 72 g of palladium-carbon catalyst was added. Hydrogen displaced air 4 times and the reaction was stirred at 5 atm hydrogen pressure for 24 hours. Filter, concentrate the solution, add 10 L of ethyl acetate to the residue, wash with water (3 L x 2), wash with 2 L of saturated brine, dry with anhydrous sodium sulfate, and evaporate the solvent at 78°C to yield 898 g of oily liquid B. (3) Add oily liquid B to a 20 L reactor, add 5 L of dimethylformamide, 184 mL of distilled water, and 299 g of sodium chloride, and reflux the reaction for 35 hrs. The reaction solution was added to 12 L of distilled water, extracted with ethyl acetate (2.5 L x 6), the organic phases were combined, washed with water (2 L x 3), washed with 2 L of saturated brine, dried with anhydrous sodium sulfate, and dried at room temperature to yield 506 g of solid C. (4) Solid C was added to a 10 L reaction flask, dissolved with 4 L of tetrahydrofuran and 2 L of distilled water, and 270 g of lithium hydroxide monohydrate was added in batches with stirring in an ice bath. Keep for 3 hours. 4 mol/L hydrochloric acid was added dropwise to pH 2-3, extracted with ethyl acetate (1 L x 3), the organic phases were combined, washed with 1 L of water, 1 L of saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was dissolved in 0.5 L of ethyl acetate, 4.5 L of petroleum ether was added slowly and stirred for 10 h at room temperature, filtered, and the filter cake was washed with petroleum ether and milled to give 380 g of solid D. (5) Solid D was added to a 5 L reaction flask, dissolved in 3 L of ethanol, and 0.5 L of ethanol solution of 425 g of L-leucinamide was added dropwise with stirring. It was heated to 50 °C and stirred for 3 h. It was cooled to room temperature and continued stirring for 3 h. It was filtered and the filter cake was washed with ethanol. The filter cake was dissolved in a mixture of 2.5 L of acetonitrile and 0.5 L of ethanol, heated to 50 °C and stirred for 2 h, cooled to room temperature and stirred for 2 h, filtered, and the filter cake was washed with acetonitrile, and milled to yield 364 g of solid E. (6) The solid E was dissolved in 3 L of distilled water, and 3 mol/L of hydrochloric acid was slowly added dropwise to pH 2-3 under stirring in an ice bath and stirring was continued for 1 hour. The reaction solution was extracted with dichloromethane (1 L x 3), and the organic phase was washed with 0.5 L saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was dissolved in a mixture of 0.25 L of ethyl acetate and 2.25 L of petroleum ether, stirred at room temperature for 2 h. It was filtered to give 149 g of solid F. (7) Solid F, 393 mL of diphenylphosphoryl azide, and 315 mL of triethylamine were added to 3 L of the reaction flask, dissolved with 2 L of tert-butanol, and stirred at reflux for 12 hours. The reaction solution was concentrated, extracted by adding 3 L of ethyl acetate, and the organic phase was washed sequentially with 400 mL of saturated ammonium chloride solution, 400 mL of saturated sodium bicarbonate solution, 300 mL of saturated brine, dried over anhydrous sodium sulfate, filtered, and the solvent was evaporated. The residue was dissolved in 800 mL of a mixture of petroleum ether and ethyl acetate (10:1), stirred for 3 h. Filtered to give 167 g of solid G. (8) Dissolved solid G and 470 g of p-toluenesulfonic acid in 3 L of acetonitrile, stirred for 36 h at room temperature. Concentrate, add 600 mL of a mixed solution of ethyl ether and petroleum ether (1:1), stir for 3 h. Filter to obtain 204 g of sitafloxacin ternary ring intermediate (purity 99.2%).

References

[1] Patent: CN104803857, 2017, B. Location in patent: Paragraph 0038-0064

(1R,2S)-Fluorocyclopropylamine tosylate Preparation Products And Raw materials

Global( 154)Suppliers
Supplier Tel Email Country ProdList Advantage
Chem-Stone Co.,Ltd. 020-82185713,82185709 13418171485 sales@chem-stone.com China 743 56
Suzhou Chukai PharmaTech 0512-88812066 wenlongfcb@qq.com China 110 62
Suzhou Chukai PharmaTech 0512-88812066 wenlongfcb@qq.com China 470 58
NanJing Jiexin chemicals Co.,Ltd 15005178685; 15005178685 1347015058@qq.com China 61 58
YITAI Pharmatech Co.,Ltd. 86-10-67806114 China 2 49
Chemvon Biotechnology Co., Ltd 021-50790412 info@chemvon.com China 371 57
Energy Chemical 400-0056266 sales8178@energy-chemical.com China 44850 61
Jia Xing Isenchem Co.,Ltd 0573-85285100 18627885956 isenchem@163.com China 9389 66
Adamas Reagent, Ltd. 400-6009262 15618770481 yhx@titansci.com China 14098 59
Shanghai Hanhong Scientific Co.,Ltd. 021-54306202 13764082696 info@hanhongsci.com China 42917 64

View Lastest Price from (1R,2S)-Fluorocyclopropylamine tosylate manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
(1R,2S)-2-fluorocyclopropanamine 4-methylbenzenesulfonate pictures 2025-04-04 (1R,2S)-2-fluorocyclopropanamine 4-methylbenzenesulfonate
143062-84-4
1kg 98% 1Ton Henan Aochuang Chemical Co.,Ltd.
(1R,2S)-FLUOROCYCLOPROPYLAMINE TOSYLATE pictures 2019-07-06 (1R,2S)-FLUOROCYCLOPROPYLAMINE TOSYLATE
143062-84-4
$100.00 1KG 98% 200KG Career Henan Chemical Co
(1R,2S)-FLUOROCYCLOPROPYLAMINE TOSYLATE pictures 2018-03-07 (1R,2S)-FLUOROCYCLOPROPYLAMINE TOSYLATE
143062-84-4
$1.00 1KG 99% 100t Shanghai Yingrui Biopharma Co., Ltd.

(1R,2S)-Fluorocyclopropylamine tosylate Spectrum

Cyclopropanamine, 2-fluoro-,(1R,2S)-,4-methylbenzenesulfonate (1R,2S)-4-Methylbenzenesulfonate-2-fluoro-CyclopropanaMine (1R,2S)-2-Fluorocyclopropanamine 4-methylbenzenesulfonate (1R,2S)-2-Fluorocyclopropylamine tosylate (1R,2S)-2-fluorocyclopropan-1-amine tosylic acid CyclopropanaMine, 2-fluoro-, (1R,2S)-, 4-Methylbenzenesulfonate (1:1) (2-fluorocyclopropyl)aMino 4-Methylbenzene-1-sulfonate (1R,2S)-2-Fluorocyclopropan-1-amine 4-methylbenzenesulphonate, (1R,2S)-2-Fluorocyclopropan-1-amine tosylate (1R,2S)-2-Fluorocyclopropan-1-amine toluene-4-sulphonate 98% (1R,2S)-2-Fluorocyclopropan-1-aMine tosylate [(1R,2S)-2-fluorocyclopropyl]azanium N-fluorocyclopropanamine 4-methylbenzenesulfonate Sitafloxacin Impurity 60 Sitafloxacin Impurity 3 Tosic acid Sitafloxacin Impurity 51 (1R, 2S) -2-fluorocyclopropylamine p-toluenesulfonic acid salt (1R,2S)-2-Fluorocyclopropan-1-amine toluene-4-sulphonate (1R,2S)-2-fluorocyclopropan-1-amine 4-methylbenzenesulfonate Sitafloxacin Impurity 26(4-Methylbenzenesulfonate) (1R,2S)-FLUOROCYCLOPROPYLAMINE TOSYLATE Sitafloxacin Compound FL0046 (1R,2S)-2-fluorocyclopropan-1-amine (1R,2S)-Fluorocyclopropylamine tosylate 143062-84-4 143062-83-4 C7H8O3SC3H6FN