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84163-13-3

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  • 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride USD200/kg Iloperidone intermediate

    Cas No: 84163-13-3

  • USD $ 200.0-245.0 / Kilogram

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84163-13-3 Usage

Uses

6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole Hydrochloride (Risperidone EP Impurity M; Paliperidone USP Related Compound B) is a novel antiproliferative agent.

Check Digit Verification of cas no

The CAS Registry Mumber 84163-13-3 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,4,1,6 and 3 respectively; the second part has 2 digits, 1 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 84163-13:
(7*8)+(6*4)+(5*1)+(4*6)+(3*3)+(2*1)+(1*3)=123
123 % 10 = 3
So 84163-13-3 is a valid CAS Registry Number.
InChI:InChI=1/C12H13FN2O.ClH/c13-9-1-2-10-11(7-9)16-15-12(10)8-3-5-14-6-4-8;/h1-2,7-8,14H,3-6H2;1H

84163-13-3 Well-known Company Product Price

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  • TCI America

  • (F0944)  6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole Hydrochloride  >98.0%(HPLC)(T)

  • 84163-13-3

  • 1g

  • 170.00CNY

  • Detail
  • TCI America

  • (F0944)  6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole Hydrochloride  >98.0%(HPLC)(T)

  • 84163-13-3

  • 5g

  • 560.00CNY

  • Detail
  • USP

  • (1491820)  Paliperidone Related Compound B  United States Pharmacopeia (USP) Reference Standard

  • 84163-13-3

  • 1491820-20MG

  • 14,309.10CNY

  • Detail

84163-13-3SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 17, 2017

Revision Date: Aug 17, 2017

1.Identification

1.1 GHS Product identifier

Product name 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride

1.2 Other means of identification

Product number -
Other names 6-fluoro-3-piperidin-4-yl-1,2-benzoxazole,hydrochloride

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:84163-13-3 SDS

84163-13-3Synthetic route

(2,4-difluorophenyl)(4-piperidinyl)methanone oxime
84163-46-2

(2,4-difluorophenyl)(4-piperidinyl)methanone oxime

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
With N-methylcyclohexylamine; potassium tert-butylate In water; toluene for 6h; Reflux;97.8%
Stage #1: (2,4-difluorophenyl)(4-piperidinyl)methanone oxime With potassium hydroxide In water; toluene for 6h; Reflux; Inert atmosphere;
Stage #2: With hydrogenchloride In ethanol; water at 70 - 80℃; Temperature;
96.33%
(2,4-Difluoro-phenyl)-piperidin-4-yl-methanone hydrochloride

(2,4-Difluoro-phenyl)-piperidin-4-yl-methanone hydrochloride

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Stage #1: (2,4-Difluoro-phenyl)-piperidin-4-yl-methanone hydrochloride With hydroxylamine hydrochloride; potassium hydroxide In methanol
Stage #2: With potassium hydroxide In methanol at 40 - 45℃; for 12h;
Stage #3: With hydrogenchloride In methanol; water at 0 - 30℃; for 2h; pH=< 1; Solvent; Reagent/catalyst; Temperature; Concentration;
90.4%
Multi-step reaction with 2 steps
1: hydroxylamine hydrochloride; N-methylcyclohexylamine / ethanol / 12 h / 60 °C
2: potassium tert-butylate; N-methylcyclohexylamine / water; toluene / 6 h / Reflux
View Scheme
6-fluoro-3-(1-formyl-4-piperidinyl)-1,2-benzisoxazole
84163-41-7

6-fluoro-3-(1-formyl-4-piperidinyl)-1,2-benzisoxazole

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
With hydrogenchloride In ethanol for 3h; Heating; Yield given;
With hydrogenchloride In methanol; ethanol; benzene1.25 g (31.8%)
With hydrogenchloride
1-formyl-4-(2,4-difluorobenzoyl)piperidine oxime
84162-94-7

1-formyl-4-(2,4-difluorobenzoyl)piperidine oxime

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: NaH / dimethylformamide / 4 h / 70 - 75 °C
2: aq. HCl / ethanol / 3 h / Heating
View Scheme
Multi-step reaction with 2 steps
1: potassium hydroxide / isopropyl alcohol; water
2: hydrogenchloride
View Scheme
6-fluoro-3-(1-methylpiperidin-4-yl)benzisoxazole
416852-17-0

6-fluoro-3-(1-methylpiperidin-4-yl)benzisoxazole

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
With 2-Chloroethyl chloroformate; triethylamine In 1,2-dichloro-ethane at 0 - 20℃;
1-formylisonipecotoyl chloride
84163-43-9

1-formylisonipecotoyl chloride

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: aluminum (III) chloride
2: hydrogenchloride; hydroxylamine hydrochloride / isopropyl alcohol; water
3: potassium hydroxide / isopropyl alcohol; water
4: hydrogenchloride
View Scheme
isonipecotic acid
498-94-2

isonipecotic acid

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1: acetic anhydride
2: thionyl chloride
3: aluminum (III) chloride
4: hydrogenchloride; hydroxylamine hydrochloride / isopropyl alcohol; water
5: potassium hydroxide / isopropyl alcohol; water
6: hydrogenchloride
View Scheme
1-Formylisonipecotic acid
84163-42-8, 67659-34-1, 67659-33-0

1-Formylisonipecotic acid

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1: thionyl chloride
2: aluminum (III) chloride
3: hydrogenchloride; hydroxylamine hydrochloride / isopropyl alcohol; water
4: potassium hydroxide / isopropyl alcohol; water
5: hydrogenchloride
View Scheme
4-(2,4-difluorobenzoyl)-1-piperidinecarboxaldehyde
84162-80-1

4-(2,4-difluorobenzoyl)-1-piperidinecarboxaldehyde

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: hydrogenchloride; hydroxylamine hydrochloride / isopropyl alcohol; water
2: potassium hydroxide / isopropyl alcohol; water
3: hydrogenchloride
View Scheme
(2,4-difluorophenyl)-piperidin-4-yl-methanone oxime hydrochloride
135634-18-3

(2,4-difluorophenyl)-piperidin-4-yl-methanone oxime hydrochloride

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Stage #1: (2,4-difluorophenyl)-piperidin-4-yl-methanone oxime hydrochloride With potassium hydroxide In methanol for 2.5h; Heating;
Stage #2: With hydrogenchloride In water; acetone at 20℃; for 0h; pH=2 - 3;
35 g
C13H15F2NO
416852-15-8

C13H15F2NO

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: hydroxylamine hydrochloride / pyridine / 60 °C
2: sodium hydride / tetrahydrofuran; N,N-dimethyl-formamide / 70 - 75 °C
3: 2-Chloroethyl chloroformate; triethylamine / 1,2-dichloro-ethane / 0 - 20 °C
View Scheme
C13H16F2N2O
416852-16-9

C13H16F2N2O

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: sodium hydride / tetrahydrofuran; N,N-dimethyl-formamide / 70 - 75 °C
2: 2-Chloroethyl chloroformate; triethylamine / 1,2-dichloro-ethane / 0 - 20 °C
View Scheme
2,4-difluorobenzaldehyde
1550-35-2

2,4-difluorobenzaldehyde

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: tetrahydrofuran / 20 °C
2: hydroxylamine hydrochloride / pyridine / 60 °C
3: sodium hydride / tetrahydrofuran; N,N-dimethyl-formamide / 70 - 75 °C
4: 2-Chloroethyl chloroformate; triethylamine / 1,2-dichloro-ethane / 0 - 20 °C
View Scheme
(1-methyl-4-piperidyl)magnesium chloride
63463-36-5

(1-methyl-4-piperidyl)magnesium chloride

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: tetrahydrofuran / 20 °C
2: hydroxylamine hydrochloride / pyridine / 60 °C
3: sodium hydride / tetrahydrofuran; N,N-dimethyl-formamide / 70 - 75 °C
4: 2-Chloroethyl chloroformate; triethylamine / 1,2-dichloro-ethane / 0 - 20 °C
View Scheme
1,3-Difluorobenzene
372-18-9

1,3-Difluorobenzene

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: aluminum (III) chloride / dichloromethane / 3 h / 20 °C
2.1: hydrogenchloride / water / 5 h / Reflux
3.1: hydroxylamine hydrochloride / ethanol / 3 h / Reflux
4.1: potassium hydroxide / water; toluene / 6 h / Reflux; Inert atmosphere
4.2: 70 - 80 °C
View Scheme
1-acetylpiperidine-4-carbonyl chloride
59084-16-1

1-acetylpiperidine-4-carbonyl chloride

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: aluminum (III) chloride / dichloromethane / 3 h / 20 °C
2.1: hydrogenchloride / water / 5 h / Reflux
3.1: hydroxylamine hydrochloride / ethanol / 3 h / Reflux
4.1: potassium hydroxide / water; toluene / 6 h / Reflux; Inert atmosphere
4.2: 70 - 80 °C
View Scheme
1-[4-(2.4-Difluoro-benzoyl)-piperidin-1-yl]-ethanone
84162-82-3

1-[4-(2.4-Difluoro-benzoyl)-piperidin-1-yl]-ethanone

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: hydrogenchloride / water / 5 h / Reflux
2.1: hydroxylamine hydrochloride / ethanol / 3 h / Reflux
3.1: potassium hydroxide / water; toluene / 6 h / Reflux; Inert atmosphere
3.2: 70 - 80 °C
View Scheme
Boc-Trp-OH
13139-14-5

Boc-Trp-OH

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

C28H31FN4O4
1270202-32-8

C28H31FN4O4

Conditions
ConditionsYield
Stage #1: Boc-Trp-OH With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
96%
4-(3-chloropropoxy)-3-methoxyacetophenone
58113-30-7

4-(3-chloropropoxy)-3-methoxyacetophenone

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

iloperidone
133454-47-4

iloperidone

Conditions
ConditionsYield
Stage #1: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With sodium hydroxide In water at 25 - 30℃; for 0.25h; Industrial scale; Green chemistry;
Stage #2: 4-(3-chloropropoxy)-3-methoxyacetophenone In water at 25 - 30℃; for 0.25h; Industrial scale; Green chemistry;
Stage #3: With tetrabutylammomium bromide In n-heptane; water at 65 - 70℃; Reagent/catalyst; Solvent; Temperature; Concentration; Time; Industrial scale; Green chemistry;
95%
With sodium hydrogencarbonate In toluene; acetonitrile at 76℃; for 6h; Temperature;90.5%
With potassium carbonate In N,N-dimethyl-formamide at 90℃; for 16h;
3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one
130049-82-0

3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

paliperidone
144598-75-4

paliperidone

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine In methanol for 24h; Reflux;94%
With N-ethyl-N,N-diisopropylamine In methanol Product distribution / selectivity; Reflux;93%
With N-ethyl-N,N-diisopropylamine In methanol at 60℃; Reagent/catalyst; Inert atmosphere;90%
3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one monohydrochloride

3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one monohydrochloride

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Risperidone
106266-06-2

Risperidone

Conditions
ConditionsYield
With sodium carbonate In methanol at 73 - 75℃; for 4 - 4.5h; Product distribution / selectivity;93.6%
With sodium carbonate In water at 25 - 55℃; for 9h; Product distribution / selectivity;
With sodium carbonate In water; acetonitrile at 25 - 75℃; for 8h; Product distribution / selectivity;
3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one
63234-80-0

3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Risperidone
106266-06-2

Risperidone

Conditions
ConditionsYield
With sodium carbonate In water at 110 - 120℃; for 0.666667h; Product distribution / selectivity;93.2%
With sodium carbonate; potassium iodide In N,N-dimethyl-formamide at 80℃; for 10h; Temperature;76.9%
N-tert-butoxycarbonyl-L-phenylalanine
13734-34-4

N-tert-butoxycarbonyl-L-phenylalanine

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

C26H30FN3O4
1270202-31-7

C26H30FN3O4

Conditions
ConditionsYield
Stage #1: N-tert-butoxycarbonyl-L-phenylalanine With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
92%
Stage #1: N-tert-butoxycarbonyl-L-phenylalanine With 4-methyl-morpholine; benzotriazol-1-ol; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
85%
3-(2-chloroethyl)-9-(methoxymethoxy)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-α]pyrimidin-4-one

3-(2-chloroethyl)-9-(methoxymethoxy)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-α]pyrimidin-4-one

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

3-(2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl)-9-(methoxymethoxy)-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-α]pyrimidin-4-one

3-(2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl)-9-(methoxymethoxy)-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-α]pyrimidin-4-one

Conditions
ConditionsYield
With potassium carbonate; potassium iodide In acetonitrile at 75 - 78℃; Reagent/catalyst;92%
6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

2-chloropropionyl chloride
625-36-5

2-chloropropionyl chloride

3-chloro-1-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)propan-1-one

3-chloro-1-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)propan-1-one

Conditions
ConditionsYield
With sodium hydroxide In dichloromethane; water at 0 - 20℃; for 5h; Large scale;91%
N-tert-butoxycarbonyl-O-2,6-dichlorobenzyl-L-tyrosine
40298-71-3

N-tert-butoxycarbonyl-O-2,6-dichlorobenzyl-L-tyrosine

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

C33H34Cl2FN3O5
1270202-33-9

C33H34Cl2FN3O5

Conditions
ConditionsYield
Stage #1: N-tert-butoxycarbonyl-O-2,6-dichlorobenzyl-L-tyrosine With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
90.9%
Stage #1: N-tert-butoxycarbonyl-O-2,6-dichlorobenzyl-L-tyrosine With 4-methyl-morpholine; benzotriazol-1-ol; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
84%
6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Boc-Gly-Gly-Ala-Pro-OH
151396-21-3

Boc-Gly-Gly-Ala-Pro-OH

C29H39FN6O7
1270202-34-0

C29H39FN6O7

Conditions
ConditionsYield
Stage #1: Boc-Gly-Gly-Ala-Pro-OH With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
90.5%
8-(3-chloropropanoyl)-5,6-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-4(2H)-one
157649-20-2

8-(3-chloropropanoyl)-5,6-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-4(2H)-one

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

8-(3-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)propanoyl)-5,6-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-4(2H)-one

8-(3-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)propanoyl)-5,6-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-4(2H)-one

Conditions
ConditionsYield
With potassium carbonate; potassium iodide In acetonitrile Reflux;89.9%
6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Boc-Gly-Val-Gly-Val-Pro

Boc-Gly-Val-Gly-Val-Pro

C36H52FN7O8
1270202-37-3

C36H52FN7O8

Conditions
ConditionsYield
Stage #1: Boc-Gly-Val-Gly-Val-Pro With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
89.1%
Boc-Glu(OBzl)-OH
13574-13-5

Boc-Glu(OBzl)-OH

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

C29H34FN3O6
1646250-75-0

C29H34FN3O6

Conditions
ConditionsYield
Stage #1: Boc-Glu(OBzl)-OH With 4-methyl-morpholine; benzotriazol-1-ol; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
89%
Boc-GFGFP-OH
1270202-28-2

Boc-GFGFP-OH

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

C44H52FN7O8
1270202-38-4

C44H52FN7O8

Conditions
ConditionsYield
Stage #1: Boc-GFGFP-OH With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
88.5%
6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Boc-Gly-Gly-Phe-Pro-OH
76046-35-0

Boc-Gly-Gly-Phe-Pro-OH

C35H43FN6O7
1270202-36-2

C35H43FN6O7

Conditions
ConditionsYield
Stage #1: Boc-Gly-Gly-Phe-Pro-OH With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
88.1%
3-(2-iodoethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one
885706-66-1

3-(2-iodoethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Risperidone
106266-06-2

Risperidone

Conditions
ConditionsYield
With potassium carbonate In acetone for 6h; Heating / reflux;87.4%
Boc-Lys(Z)-OH
2389-45-9

Boc-Lys(Z)-OH

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

C31H39FN4O6
1646250-76-1

C31H39FN4O6

Conditions
ConditionsYield
Stage #1: Boc-Lys(Z)-OH With 4-methyl-morpholine; benzotriazol-1-ol; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
87%
6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

Boc-Gly-Gly-Ile-Pro-OH
397244-47-2

Boc-Gly-Gly-Ile-Pro-OH

C32H45FN6O7
1270202-35-1

C32H45FN6O7

Conditions
ConditionsYield
Stage #1: Boc-Gly-Gly-Ile-Pro-OH With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.166667h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
86%
BOC-glycine
4530-20-5

BOC-glycine

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

C19H24FN3O4
1426224-71-6

C19H24FN3O4

Conditions
ConditionsYield
Stage #1: BOC-glycine With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.25h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
85%
Boc-Lys(Boc)-OH
2483-46-7

Boc-Lys(Boc)-OH

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

di‐tert‐butyl {6‐[4‐(6‐fluorobenzo[d]isoxazol‐3‐yl)piperidin‐1‐yl]‐6‐oxohexane‐1,5‐diyl}dicarbamate

di‐tert‐butyl {6‐[4‐(6‐fluorobenzo[d]isoxazol‐3‐yl)piperidin‐1‐yl]‐6‐oxohexane‐1,5‐diyl}dicarbamate

Conditions
ConditionsYield
Stage #1: Boc-Lys(Boc)-OH; 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 20℃; pH=8;
Stage #2: With potassium hydrogencarbonate In water for 0.5h; Cooling with ice;
85%
4-(3-chloropropoxy)-3-methoxyacetophenone
58113-30-7

4-(3-chloropropoxy)-3-methoxyacetophenone

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

iloperidone

iloperidone

Conditions
ConditionsYield
With potassium carbonate; potassium iodide In ethyl acetate; N,N-dimethyl-formamide at 80℃; for 50h; Inert atmosphere;84.65%
6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

toluene-4-sulfonic acid 2-(4-(3-piperidinopropoxy)phenyl)ethyl ester
409127-88-4

toluene-4-sulfonic acid 2-(4-(3-piperidinopropoxy)phenyl)ethyl ester

6-fluoro-3-(1-(4-(3-(piperidinyl-1-yl)propoxy)phenethyl)piperidinyl-4-yl)benzo[d]isoxazole

6-fluoro-3-(1-(4-(3-(piperidinyl-1-yl)propoxy)phenethyl)piperidinyl-4-yl)benzo[d]isoxazole

Conditions
ConditionsYield
With potassium carbonate In acetonitrile for 6h; Reflux;83.2%
tert-butyl 4-(2,4-difluorobenzoyl)piperidine-1-carboxylate
1159825-99-6

tert-butyl 4-(2,4-difluorobenzoyl)piperidine-1-carboxylate

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

C29H33F2N3O4

C29H33F2N3O4

Conditions
ConditionsYield
With potassium carbonate In 1,4-dioxane at 90℃;83%
4-(3-bromopropoxy)benzaldehyde
17954-81-3

4-(3-bromopropoxy)benzaldehyde

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

4-(3-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)propoxy)benzaldehyde

4-(3-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)propoxy)benzaldehyde

Conditions
ConditionsYield
With potassium carbonate In acetonitrile for 6h; Reflux;82.4%
1-(tert-butoxycarbonyl)-L-proline
15761-39-4

1-(tert-butoxycarbonyl)-L-proline

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

tert-butyl 2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-carbonyl)pyrrolidine-1-carboxylate
1426224-72-7

tert-butyl 2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-carbonyl)pyrrolidine-1-carboxylate

Conditions
ConditionsYield
Stage #1: 1-(tert-butoxycarbonyl)-L-proline With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 0℃; for 0.25h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With 4-methyl-morpholine In N,N-dimethyl-formamide at 0 - 20℃; pH=8;
82%
C11H14ClN3O2
1204248-71-4

C11H14ClN3O2

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

C23H26FN5O3
1204248-69-0

C23H26FN5O3

Conditions
ConditionsYield
With sodium hydrogencarbonate In methanol; N,N-dimethyl-formamide at 70 - 90℃; for 8h; Inert atmosphere;81.8%
rac-5-methanesulfonyl-2-(2,2,2-trifluoro-1-methylethoxy)benzoic acid

rac-5-methanesulfonyl-2-(2,2,2-trifluoro-1-methylethoxy)benzoic acid

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride
84163-13-3

6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride

(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)(5-(methylsulfonyl)-2-((1,1,1-trifluoropropan-2-yl)oxy)phenyl)methanone

(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)(5-(methylsulfonyl)-2-((1,1,1-trifluoropropan-2-yl)oxy)phenyl)methanone

Conditions
ConditionsYield
Stage #1: rac-5-methanesulfonyl-2-(2,2,2-trifluoro-1-methylethoxy)benzoic acid With N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane at 20℃; for 0.5h;
Stage #2: 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride With triethylamine In dichloromethane at 20℃;
81%

84163-13-3Relevant articles and documents

Purification method of 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride

-

, (2021/04/10)

The invention discloses a purification method of a risperidone intermediate 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride as shown in a formula II, which is characterized by comprising the following steps: adding 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride into ethanol, adding a certain amount of water, and carrying out heating reflux until the solution is clear to obtain the risperidone intermediate 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride; and cooling the compound to a certain temperature for crystal growing, then cooling the mixture to -5 to 10 DEG C, and filtering and drying the mixture to obtain the crystal. According to the purification method of the 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole hydrochloride, the dimer shown as the formula V can be effectively separated out, the purification yield is 85% or above, the chemical purity of a finished product can reach 99.9% or above, an amplification effect cannot be generated in large-scale production, and the process is stable.

Preparation method of risperidone

-

Paragraph 0030-0037, (2019/04/02)

The invention discloses a preparation method of risperidone, and belongs to the technical field of preparation methods for chemical medical intermediates. High-purity risperidone is prepared by performing oximation, cyclization and condensation reactions on 2,4- difluorophenyl-4,-piperidone methanone hydrochloride and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyridino-[1,2-a]pyridine-4-ketone as raw materials. The method disclosed by the invention has the advantages of adoption of relatively cheap and readily-available raw materials, easiness in operation, higher yield and higher industrial value.

PIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF

-

Page/Page column 36, (2008/12/08)

The present invention relates to Compounds of Formula (I), compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IFG) in a patient.

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