PROCESS FOR PRODUCING (Œ)-trans-4-(4-FLUOROPHENYL)-3-HYDROXYMETHYLPIPERIDINE

PROCESS FOR PRODUCING (Œ)-trans-4-(4-FLUOROPHENYL)-3-HYDROXYMETHYLPIPERIDINE

PROBLEM TO BE SOLVED: To provide a process by which (±)-trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidine can simply and industrially be produced in good purity and good yield. SOLUTION: The process for producing the (±)-trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidine is carried out as follows....

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Hauptverfasser: YAMADA SEIJI, ISHIHARA AKIRA, KAWAMI KO
Format: Patent
Sprache:eng
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APPARATUS THEREFOR
CHEMISTRY
GENERAL METHODS OF ORGANIC CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator YAMADA SEIJI
ISHIHARA AKIRA
KAWAMI KO
description PROBLEM TO BE SOLVED: To provide a process by which (±)-trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidine can simply and industrially be produced in good purity and good yield. SOLUTION: The process for producing the (±)-trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidine is carried out as follows. (±)-trans-4-(4-Fluorophenyl)-3-methoxycarbonylpiperidin-6-one is reduced with a boron trifluoride-ether complex and sodium borohydride to provide a reaction solution. A mineral acid and a potassium salt are then added to the resultant reaction solution to regulate the pH to 0.5-4.0. Deposited materials are removed to afford an acidic solution. The pH of the resultant acidic solution is then regulated to 11.0-12.5. COPYRIGHT: (C)2008,JPO&INPIT
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SOLUTION: The process for producing the (±)-trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidine is carried out as follows. (±)-trans-4-(4-Fluorophenyl)-3-methoxycarbonylpiperidin-6-one is reduced with a boron trifluoride-ether complex and sodium borohydride to provide a reaction solution. A mineral acid and a potassium salt are then added to the resultant reaction solution to regulate the pH to 0.5-4.0. Deposited materials are removed to afford an acidic solution. The pH of the resultant acidic solution is then regulated to 11.0-12.5. 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SOLUTION: The process for producing the (±)-trans-4-(4-fluorophenyl)-3-hydroxymethylpiperidine is carried out as follows. (±)-trans-4-(4-Fluorophenyl)-3-methoxycarbonylpiperidin-6-one is reduced with a boron trifluoride-ether complex and sodium borohydride to provide a reaction solution. A mineral acid and a potassium salt are then added to the resultant reaction solution to regulate the pH to 0.5-4.0. Deposited materials are removed to afford an acidic solution. The pH of the resultant acidic solution is then regulated to 11.0-12.5. 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subjects APPARATUS THEREFOR
CHEMISTRY
GENERAL METHODS OF ORGANIC CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title PROCESS FOR PRODUCING (Œ)-trans-4-(4-FLUOROPHENYL)-3-HYDROXYMETHYLPIPERIDINE
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