Afatinib N-2, CAS Number 314771-76-1

Basic Info

Model No.:  314771-76-1

Additional Info

Packaging: AS REQUIRED

Productivity: KGS

Brand: VOLSENCHEM

Transportation: Air,DHL

Place of Origin: CHINA

Supply Ability: TRUE MANUFACTURER

Certificate: ISO

Product Description

Afatinib minus two intermediate, we referred it as afatinib N-2, CAS number is 314771-76-1, which is a high-level intermediate of afatinib, later only through two steps reaction to get afatinib. There are two main synthesis ideas in the literature, the first, put the bromo crotonic acid and oxalyl chloride take reaction to get the acid chloride and then process acylation with afatinib N-2, followed by adding dimethylamine to obtain afatinib. This method yield up to only 50%, in addition need the separation by column chromatography, does not suitable to commercial production. The second, dimethylaminocrotonic acid hydrochloride through the amide connection reagent 1,1-carbonyldiimidazole activation or chlorination and acted with afatinib N-2 to get afatinib, This method must require activation of the methyl crotonic acid hydrochloride, then carry out the subsequent condensation reaction, the steps are increased, and the yield of the product is low. There is a more reliable synthesis method, use tetrabromide and organic phosphorus compounds as the condensation reagent, dimethylaminocrotonic acid and afatinib N-2 as raw materials, carry out the condensation reaction to get afatinib, this method broaden the range of selection of the condensation reagent during the preparation, the result shows the yield is high and purity is perfect.

Thera. Category:Anti- cancer

Cas No.:  314771-76-1

Synonym: Afatinib-des(4-dimethylamino-2-en-1-oxo)butyl;Intermediates of sunitinib;(S)-N4-(3-chloro-4-fluorophenyl)-7-(tetrahydrofuran-3-yloxy)quinazoline-4,6-diaMine;N4-(3-Chloro-4-fluorophenyl)-7-[[(3S)-tetrahydro-3-furanyl]oxy]-4,6-quinazolinediamine;7-((S)-tetrahydrofuran-3-yloxy)-4-(3-chloro-4-fluorophenyl) aMino-6-aMinoquinazoline;Afatinib IMpurity B

Molecular Formula: C18H16ClFN4O2

Molecular Weight:374.7966432

Assay: ≥98.%

Packing: Export worthy packing

Material Safety Data Sheet: Available on request

Usage: Intermediate of Afatinib

Related Intermediates :
1. CAS 162012-69-3, 7-Fluoro-6-nitro-4-hydroxyquinazoline
2. CAS 16499-57-3, 7-Fluoroquinazolin-4(3H)-one

         3. CAS 162012-67-1, 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro- ,

         4. 4-QuinazolinaMine, N-(3-chloro-4-fluorophenyl)-6-nitro-7-[[(3S)-tetrahydro-3-furanyl]oxy]- is afatinib intermediate with the    CAS number 314771-88-5, 

        5. (S)-N4-(3-chloro-4-fluorophenyl)-7-(tetrahydrofuran-3-yloxy)quinazoline-4,6-diaMine CAS 314771-76-1

        6.  3095-95-2,Diethylcarboxymethylphosphonate