A kind of preparation method of paroxetine hydrochloride key intermediate

A technology of paroxetine hydrochloride and intermediates, which is applied in the field of drug synthesis, can solve problems such as environmental pollution and waste, and achieve the effects of improving enterprise benefits and reducing input costs.
CN109020872BActive Publication Date: 2020-05-12ZHEJIANG HUABANG MEDICAL & CHEM
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG HUABANG MEDICAL & CHEM
Publication Date
2020-05-12

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Abstract

The invention discloses a preparation method of a key intermediate of paroxetine hydrochloride. The preparation method comprises: carrying out benzyl site halogenation on (+)-trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine as a starting material through a halogenation reagent to obtain a compound II, carrying out an elimination reaction process on the compound II to obtain a compound III, and carrying out catalytic hydrogenation reduction on the compound III to obtain (+)-trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine. The preparation method can convert a by-product (+)-trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine, which cannot be directly utilized, into (+ / -)-trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine. The product can be directly used as an intermediate for synthesizing paroxetine hydrochloride, change wastes into valuables, improve the benefits of enterprises and reduce the input cost of the enterprise.
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Description

technical field

[0001] The invention belongs to the field of drug synthesis, and in particular relates to a key intermediate of paroxetine hydrochloride (+)-trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine through a chemical method A synthetic method for conversion to (±)-trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine. . Background technique

[0002] Paroxetine hydrochloride is a drug developed by GlaxoSmithKline to treat various types of depression, including depression accompanied by anxiety and reactive depression. It was first launched in 1992. At present, there is a key intermediate (±)-trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine racemate in the process of synthesizing paroxetine hydrochloride, but the synthesis Paroxetine hydrochloride only needs (-) trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine, because only this spatial configuration is effective, if (+)- If trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpipe...

Claims

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