6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole Chemical Properties

Melting point:

59-62°C

Boiling point:

359.0±42.0 °C(Predicted)

Density 

1.216±0.06 g/cm3(Predicted)

storage temp. 

Keep in dark place,Inert atmosphere,Room temperature

solubility 

Chloroform (Slightly), Methanol (Slightly)

pka

9.74±0.10(Predicted)

form 

Solid

color 

White to Off-White

Stability:

Hygroscopic

CAS DataBase Reference

84163-77-9(CAS DataBase Reference)

Safety Information

Hazard Codes 

T

Risk Statements 

25-36/37/38

Safety Statements 

45-26

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

HazardClass 

IRRITANT

HS Code 

29349990

6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole Usage And Synthesis

Chemical Properties

White Crystalline Powder

Uses

An Intermediate in the synthesis of risperidone and iloperidone.

Synthesis

The general procedure for the synthesis of 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole from (2,4-difluorophenyl)-(4-piperidinyl)methanone oxime hydrochloride (5.52 g, 20 mmol) is as follows: The raw material was added to 25 mL of 50% potassium hydroxide solution and the reaction was carried out at reflux for 4 hours. After completion of the reaction, it was cooled to room temperature and extracted with toluene (25 mL × 2). The organic phases were combined, dried with anhydrous magnesium sulfate, filtered and concentrated to dryness under reduced pressure. The crude product was recrystallized in ether to give 3.3 g of the target product in 75% yield.

References

[1] Patent: EP2322520, 2011, A1. Location in patent: Page/Page column 16
[2] Patent: JP5714152, 2015, B2. Location in patent: Paragraph 0089

6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole(84163-77-9)Related Product Information

• 3-(4-Piperidinyl)-1,2-benzisoxazole Hydrochloride
• Iloperidone Diketo Impurity
• (2-FLUORO-PHENYL)-PIPERIDIN-4-YL-METHANONE
• Desfluoro Iloperidone (IMpurity)
• ILOPERIDONE
• DROPERIDOL
• Benperidol
• Haloperidol
• 5-FLUORO-3-(4-PIPERIDINYL)-1,2-BENZISOXAZOLE HYDROCHLORIDE
• 6-phenyl-1H-pyrrolo[2,3-b]pyridine
• 5-FLUORO-3-(4-PIPERIDINYL)-1,2-BENZISOXAZOLE
• Iloperidone Carboxylic Acid
• Ethanone, 1-(3-hydroxy-2-methoxyphenyl)- (9CI)
• Hydroxy Iloperidone
• (E)-4-(2,4-Difluorobenzoyl)piperidine OxiMe
• Iloperidone iMpurity
• Iloperidone Impurity 21
• 3-Piperidin-4-ylbenzo[d]isoxazole