![](/CAS/20200611/GIF/1231930-48-5.gif)
N-[5-[(4-Boc-1-piperazinyl)methyl]-2-pyridyl]-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-6-benzimidazolyl)pyrimidin-2-amine synthesis
- Product Name:N-[5-[(4-Boc-1-piperazinyl)methyl]-2-pyridyl]-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-6-benzimidazolyl)pyrimidin-2-amine
- CAS Number:1231930-48-5
- Molecular formula:C30H36F2N8O2
- Molecular Weight:578.66
![1H-BenziMidazole, 6-(2-chloro-5-fluoro-4-pyriMidinyl)-4-fluoro-2-Methyl-1-(1-Methylethyl)-](/CAS/20150408/GIF/1231930-42-9.gif)
1231930-42-9
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$12.00/100mg
![tert-butyl 4-((6-aminopyridin-3-yl)methyl)piperazine-1-carboxylate](/CAS/20180703/GIF/1178566-52-3.gif)
1178566-52-3
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![N-[5-[(4-Boc-1-piperazinyl)methyl]-2-pyridyl]-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-6-benzimidazolyl)pyrimidin-2-amine](/CAS/20200611/GIF/1231930-48-5.gif)
1231930-48-5
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Yield:1231930-48-5 87%
Reaction Conditions:
with tris-(dibenzylideneacetone)dipalladium(0);Cs2CO3;4,5-bis(diphenylphosphino)-9,9-dimethylxanthene in tert-butyl alcohol at 110; for 8 h;Inert atmosphere;
Steps:
5.2 tert-butyl 4-((6-((5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-yl)amino)pyridin-3-yl)methyl)piperazine-1-carboxylate (2-20)
To a suspension of 6-(2-chloro-5-fluoropyrimidin-4-yl)-4-fluoro-l-isopropyl-2- methyl-lH-benzo[d]imidazole (2-18, 258 mg, 0.8 mmol), tert-butyl 4~((6~aminopyridin-3- yl)methyl)piperazine-l-carboxylate (2-19, 350.6 mg, 1.2 mmol) and Cs2COs (782 mg, 2.4 mmol) in 5 mL of -BuOH were added Pd2(dba)3 (73.3 mg, 0.08 mmol) and Xantphos (23 mg, 0.04 mmol) under an atmosphere of N2. The mixture was heated to i l0°C and stirred for 8h. The mixture was then cooled to room temperature, extracted with CHCta and isopropanoi (V7V=4: 1), and the combined organic layers were washed with brine, dried over anhydrous Na2S04, filtered, and concentrated under reduced pressure. The crude product was purified by column chromatography on silica gel (0-10% MeOH in DCM) to give fe/ -butyl 4-((6-(5- fluoro-4-(4-fluoro-l-isopropyl-2-memyl-lH-benzo|"d]inudazol-6-yl)pyrimidin-2- ylamino)pyridin-3-yl)methyl)piperazine-l-carboxyiate 2-20 as a white solid (403 mg, 87%). LCMS: m/z 579,3 [M+ 1 ] .
References:
WO2017/185031,2017,A1 Location in patent:Page/Page column 96; 97
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1231930-37-2
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$20.00/100mg
![N-[5-[(4-Boc-1-piperazinyl)methyl]-2-pyridyl]-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-6-benzimidazolyl)pyrimidin-2-amine](/CAS/20200611/GIF/1231930-48-5.gif)
1231930-48-5
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57260-71-6
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![N-[5-[(4-Boc-1-piperazinyl)methyl]-2-pyridyl]-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-6-benzimidazolyl)pyrimidin-2-amine](/CAS/20200611/GIF/1231930-48-5.gif)
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3167-49-5
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![N-[5-[(4-Boc-1-piperazinyl)methyl]-2-pyridyl]-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-6-benzimidazolyl)pyrimidin-2-amine](/CAS/20200611/GIF/1231930-48-5.gif)
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![N-[5-[(4-Boc-1-piperazinyl)methyl]-2-pyridyl]-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-6-benzimidazolyl)pyrimidin-2-amine](/CAS/20200611/GIF/1231930-48-5.gif)
1231930-48-5
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