ChemicalBook CAS DataBase List Tucatinib

Tucatinib synthesis

7synthesis methods

Product Name:Tucatinib
CAS Number:937263-43-9
Molecular formula:C26H24N8O2
Molecular Weight:480.52

Tukysa (Tucatinib) Tucatinib/Tucatinib (ONT-380) is an oral TKI (tyrosine kinase) inhibitor for the treatment of adult patients with advanced HER2-positive breast cancer. It can be prepared from 1-(4-((4-([ 1 ,2,4]Triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)amino)quinazolin-6-yl)-3- (1-hydroxy-2-methylpropan-2-yl)thiourea in tetrahydrofuran under basic conditions and ptoluenesulfonyl chloride through ring closure reaction.

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Yield:937263-43-9 96%

Reaction Conditions:

with p-toluenesulfonyl chloride;sodium hydroxide in tetrahydrofuran

Steps:

[001 53j Step 2: 1 -(4-((4-([ 1 ,2,4]Triazolo [1,5 -a]pyridin-7-yloxy)-3 -methylphenyl) amino)quinazolin-6-yl)-3-( 1 -hydroxy-2-methylpropan-2-yl)thiourea was agitated in tetrahydrofuran under basic conditions (2.5N NaOH), followed by the addition ofptoluenesulfonyl chloride. Water was charged to yield N4-(4-([ 1 ,2,4]triazolo [1,5 -a]pyridin-7- yloxy)-3 -methylphenyl)-N6-(4,4-dimethyl-4,5 -dihydrooxazol-2-yl)quinazoline-4,6-diamine (96%) as a mixture of polymorphs (generally a mixture containing one or more of Form C,

References:

ARRAY BIOPHARMA INC.;LEE, Patrice, A.;WINSKI, Shannon, L.;KOCH, Kevin WO2013/142875, 2013, A1 Location in patent:Paragraph 00153

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937263-44-0 Synthesis