938185-06-9Relevant articles and documents
Preparation method of erlotinib hydrochloride
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, (2020/04/01)
The invention relates to a preparation method for erlotinib hydrochloride. The preparation method comprises the following steps: reacting 2-amino-4,5-dimethoxybenzoic acid with formamide to generate acompound 5, carrying out a bromination reaction on the compound 5, and subjecting a bromination product and 3-acetenyl aniline to a reaction and amination to generate a compound 3; and reacting the compound 3 with 48% hydrobromic acid under the action of a catalyst to obtain a compound 2, and reacting the compound 2 with iodoethylmethyl ether under the action of an alkali and the catalyst to generate erlotinib hydrochloride. The method has the advantages of mild conditions, low impurity content, safety, no pollution and environmental protection, and is suitable for industrial production.
Novel method for preparing Erlotinib and intermediates thereof
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Paragraph 0050-0052, (2018/10/04)
The invention discloses a novel method for preparing Erlotinib and intermediates thereof and belongs to the field of drug synthesis. The method comprises the following steps: enabling triacetenyl aniline to react with trimethyl orthoformate or triethyl orthoformate in a proper solvent, so as to obtain a compound B; enabling the compound B and a compound C to subject to ring closing in the presenceof a proper catalyst, thereby obtaining the Erlotinib or intermediates thereof. According to the method provided by the invention, the synthesis route is short, the two-step synthesis of the target product, i.e., the Erlotinib is achieved, the consumption of high-pollution raw materials is avoided, the yield is high, the product purity is high, and thus, the method is applicable to industrial production.
NOVEL FLUORINATED DERIVATIVES AS EGFR INHIBITORS USEFUL FOR TREATING CANCERS
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Paragraph 00193-00196, (2016/09/22)
A novel class of fluorinated derivatives of Formula I have been prepared and found to be useful in the treatment of cancers and other EGFR related disorders.