Pyrazolo[3, 4-d]pyrimidin-3-one derivative, and pharmaceutical composition and application thereof
A technology of derivatives and compounds, applied to pyrazolo[3,4-d]pyrimidin-3-one derivatives, their pharmaceutical compositions and application fields, can solve problems such as drug listing
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Examples
Embodiment 1
[0314] Example 1: 6-(-2H- allyl -6-((4-(4- methylpiperazine -1- yl) phenyl) amino) -3- oxo -2,3- dihydro -1H- pyrazolo [3,4-d] pyridine -1- yl) -4- ethyl
[0315]
[0316] Step 1: Intermediate 1.1(298mg, 0.79mmol), 2- allyl -6- (methylthio) -1H- pyrazolo [3,4-d] pyrimidine -3(2H)- one (137mg, 0.72mmol), N,N'- dimethylethylenediamine (N-dimethylethylenediamine) The reaction solution was cooled to room temperature and filtered. The filter cake was washed with ethyl acetate. The filtrates were combined and concentrated under reduced pressure. The residue was purified by prep-TLC (petroleum ether / ethyl acetate = 1 / 1) to obtain compound 1(270mg) as yellow oil. m / z:[M+H] + 399.2。
[0317] Step 2: m-chloroperoxybenzoic acid (71mg, 0.35mmol) was added to the toluene (5mL) solution of Compound 1(70mg, 0.18mmol). After the reaction solution was stirred at room temperature for 1 hour, 4-(4- methylpiperazine) aniline (67mg, 0.35mmol) and N,N- diisopropylethylamine (45mg) The reaction system...
Embodiment 2～73
[0318] Examples 2 ~ 73: Synthesis of Compounds 1-2 ~ 1-73
[0319] With the synthetic method of compound 1-1, Using intermediates 1.2 ~ 1.12, 2.1 ~ 2.7, 2.15, 2-9 ~ 2.11, 2.13, 3.1 ~ 3.6, 4.14 ~ 4.16, 4.4, 4.5, 4.17, 4.21, 4.22, 4.12, 4.1 4.2, 4.35, 4.8, 4.27 ~ 4.31, 4.3, 4.32, 4.20, 4.9, 4.37, 4.10, 4.38, 4.39, 4.11, 4.40, 4.41 or 1.13 to obtain compounds 1-2 ~ 1-73.
[0320]
[0321] Table 5:
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[0323]
[0324]
[0325]
[0326]
[0327]
[0328]
[0329]
[0330]
[0331]
[0332]
Embodiment 75～85
[0333] Examples 75 ~ 85: Synthesis of Compounds 2-1 ~ 2-11
[0334] Using the synthetic method of compound 1-1, using intermediates 1.1, 1.3, 1.13, 1.2, 1.4, 1.10, 2.1, 2.2, 2.15, 3.1 and 4.34 as starting materials, the 4-(4- methylpiperazine) aniline in step 2 was replaced with 3- methoxy-4-.
[0335]
[0336] Table 6:
[0337]
[0338]
PUM
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