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Synthesis method of erlotinib hydrochloride

A technology of erlotinib hydrochloride and a synthesis method, applied in the field of drug synthesis, can solve the problems of being unsuitable for industrial production and high production cost of erlotinib hydrochloride, and achieve the effects of low production cost, easy operation and reasonable design

Inactive Publication Date: 2017-07-18
YANCHENG TEACHERS UNIV +1
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Problems solved by technology

The production cost of preparing erlotinib hydrochloride in the prior art is relatively high, and is not suitable for industrialized production

Method used

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  • Synthesis method of erlotinib hydrochloride
  • Synthesis method of erlotinib hydrochloride
  • Synthesis method of erlotinib hydrochloride

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Embodiment Construction

[0037] The technical solution of this patent will be described in further detail below in conjunction with specific embodiments.

[0038] See Figure 1-2 , A synthetic method of erlotinib hydrochloride, comprising the following steps:

[0039] (1) The first stage: preparing 3-methoxy-4-hydroxybenzonitrile from vanillin and hydroxylamine hydrochloride

[0040] Add vanillin and hydroxylamine hydrochloride to the reactor R0101 respectively, add the solvent DMF to dissolve the raw materials under stirring, and pass high-pressure steam S601001 to heat the reactor R0101. The raw materials are stirred and refluxed in the reactor R0101 for 2h, and the detection port 01001 Check the material composition, the reaction kettle stops heating reaction; then pass the condensed water CWS01002 into the reaction kettle R0101, when the temperature of the reaction solution drops to about 85℃, transfer the reaction solution to the crystallization kettle C0101, and add industrial water to the crystalliza...

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Abstract

The invention discloses a synthesis method of erlotinib hydrochloride. The synthesis method comprises the following steps: (1) at a first working section: preparing 3-methoxyl-4-hydroxybenzonitrile from vanillin and hydroxylammonium chloride; (2) at a second working section: synthesizing 3,4-dihydroxybenzonitrile; (3) at a third working section: synthesizing 3,4-di(2-methoxyethoxy)phenylacetonitrile; (4) at a fourth section: synthesizing 4,5-di(2-methoxyethoxy)-2-nitrophenylacetonitrile; (5) at a fifth working section: synthesizing 4,5-di(2-methoxyethoxy)-2-aminophenylacetonitrile hydrochloride; and (6) at a sixth working section: synthesizing the erlotinib hydrochloride. The synthesis method of the erlotinib hydrochloride, disclosed by the invention, has the advantages of reasonable design, easiness of obtaining raw materials, relatively low production cost, simplicity and easiness of operation and is suitable for industrial production.

Description

Technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a synthetic method of erlotinib hydrochloride. Background technique [0002] Erlotinib Hydrochloride (Erlotinib Hydrochloride), trade name Tarceva, is an epidermal growth factor tyrosine kinase inhibitor jointly developed by Roche, Océ Biopharmaceuticals and Genentech Pharmaceuticals. It is currently mainly used clinically Treatment of locally advanced and metastatic non-small cell lung cancer. The production cost of erlotinib hydrochloride prepared by the prior art is relatively high and is not suitable for industrialized production. Summary of the invention [0003] The purpose of the present invention is to provide a method for synthesizing erlotinib hydrochloride to solve the problems raised in the background art. [0004] In order to achieve the above objectives, the present invention provides the following technical solutions: [0005] A synthetic method of erlotinib hydroc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/94
CPCC07D239/94
Inventor 韩清顾惠雯眭靖娇殷子健孙雅泉
Owner YANCHENG TEACHERS UNIV
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