Tucatinib synthesis
- Product Name:Tucatinib
- CAS Number:937263-43-9
- Molecular formula:C26H24N8O2
- Molecular Weight:480.52
1429755-58-7
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937263-43-9
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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