ChemicalBook CAS DataBase List 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride

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

10synthesis methods

Product Name:6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride
CAS Number:84163-13-3
Molecular formula:C12H14ClFN2O
Molecular Weight:256.7

2,4-Difluorophenyl-(4-piperidinyl)methanoneoxime

84163-46-2
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6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride

84163-13-3
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$10.00/1g

Yield:84163-13-3 97.8%

Reaction Conditions:

with N-methylcyclohexylamine;potassium tert-butylate in water;toluene for 6 h;Reflux;

Steps:

5; 6; 7; 8 Example 8Preparation of 6-fluoro-3-(4-piperidinyl)-1,2-benzisazole hydrochloride (IV).
In a 1000 mL sealed four-mouth reaction bottle,Add 48.1 g of 2,4-difluorophenyl-4-piperidinone oxime (III),Potassium tert-butoxide 44.9 g,250 mL of water and 250 mL of toluene,Stir and heat to reflux for 6 h.The reaction solution is cooled to 5 to 10 ° C,Liquid separation,The aqueous layer was extracted with 250 mL of toluene.The toluene phases were combined in a 1000 mL four-necked flask.Slowly add hydrochloric acid to adjust the pH to 2~3.A large amount of white solid precipitated,Stop stirring,Filtered white solid6-fluoro-3-(4-piperidinyl)-1,2-benzisazole hydrochloride (IV) 50.2 g, yield 97.8%.

References:

Zhejiang University Of Technology Shangyu Institute Co., Ltd.;Fang Biao;Ke Junliang;Xu Meng CN109438443, 2019, A Location in patent:Paragraph 0030-0037

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