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A lapatinib and compound technology, which is applied in the preparation field of lapatinib, can solve problems to be improved, etc., and achieve the effects of mild reaction conditions and simple process operation.
Active Publication Date: 2012-09-19
HUBEI BIO PHARMA IND TECHCAL INST
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Problems solved by technology
[0005] However, the synthetic method o
Method used
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Embodiment 1
[0091] Step (1) condensation reaction:
[0092] 2-Amino-5-bromobenzonitrile (100 g, 0.508 mol) and DMF-DMA (72.7 g, 0.610 mol) were stirred and mixed, heated to 40 degrees Celsius for 4 hours, the reaction solution was concentrated to dryness under reduced pressure, and petroleum ether was added 2400ml was stirred and crystallized, filtered, and dried to obtain compound 3 as a solid (110 g, 0.437 mol), with a yield of 86.0%.
[0096] 2-Amino-5-bromobenzonitrile (100 grams, 0.508 moles) and DMF-DMA (180 grams, 1.51 moles) were stirred and mixed, heated to 75 degrees Celsius for 2 hours, the reaction solution was concentrated to dryness under reduced pressure, and a mixed solvent was added 2000 ml (the volume ratio of petroleum ether and methyl tert-butyl ether is 4:1) was stirred for crystallization, filtered, and dried to obtain compound 3 as a solid (116 g, 0.460 mol), with a yield of 90.6%.
Embodiment 3
[0098] Step (1) condensation reaction:
[0099] 2-Amino-5-bromobenzonitrile (100 g, 0.508 mol) and DMF-DMA (300 g, 2.52 mol) were stirred and mixed, heated to 60 degrees Celsius for 1 hour, the reaction solution was concentrated to dryness under reduced pressure, and ethyl 1600 ml of tert-butyl ether was stirred and crystallized, filtered, and dried to obtain compound 3 as a solid (118 g, 0.468 mol), with a yield of 92.1%.
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Abstract
The invention relates to a preparation method of Lapatinib. The method comprises the steps of carrying out condensation, cyclization, reduction, addition, twice Suzuki reaction, deprotection, addition, condensation, Boc protection removal and salification reaction on 2-amino-5-bromobenzylcyanide and 5-bromo furan-2-carboxylic acid methyl ester as starting raw materials to obtain Lapatinib. The method is easily available in starting raw materials, simple in process operation and mild in reaction conditions and does not need specific reaction equipment; in the preparation process, no compounds difficult to separate exist, and the obtained intermediates and finished product can be obtained by recrystallization; and the method is suitable for industrialized amplification production.
Description
technical field [0001] The invention belongs to the field of medicine, and in particular relates to a preparation method of lapatinib. Background technique [0002] Lapatinib (lapatinib, compound 1), the chemical name is N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-( Methanesulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine di-p-toluenesulfonate monohydrate, the chemical structure is as follows. [0003] [0004] Lapatinib is a small molecule kinase inhibitor that can simultaneously target human epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor-2 (HER2), developed by GlaxoSmithKline in 2007 Approved by the US FDA in March 2019, it is used for combination therapy: combined with capecitabine for the treatment of advanced or metastatic breast cancer overexpressing HER2, and combined with letrozole for the treatment of postmenopausal menopausal breast cancer with overexpressed HER2 and hormone receptor positive women. [00...
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