Novel synthetic method of CDK-4/6 inhibitor
A technology of CDK-4 and inhibitors, which is applied in the medical industry, can solve the problems of many reaction steps, demanding reaction equipment, and harsh reaction conditions, and achieve the effects of simple operation, low synthesis process cost, and shortened reaction steps
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[0011] The synthetic route of the specific embodiment of the present invention is as follows:
[0012] The synthesis steps are:
[0013] 1. Take 1 mol of compound 12,4-dichloro, 5-acetylpyrimidine and 1.1 mol of cyclopentylamine, add two equivalents of triethylamine in ethyl acetate, stir at room temperature, TLC shows that the reaction of the raw materials is complete, the reaction system Add water, separate the liquids, concentrate the organic phase to 80%, lower the temperature to room temperature, and then cool to 0°C, filter with suction and wash twice with cold petroleum ether to obtain the white crystal compound 2 2-chloro-4-cyclopentylamine 5-acetyl pyrimidine, yield 86%; 1 H NMR (300 MHz, CDCl3) 8.21 (s, 1H), 4.7 (b, 1H), 2.65 (m, 1H), 2.55 (s, 3H), 1.88 (m, 4H), 1.77 (m, 4H). MS: m / z = 240.6 (M+H) + ;
[0014] 2. Take 1 mol of compound 3 fructose and melt it in anhydrous tetrahydrofuran, cool to between zero and minus five degrees, add 1.9 equivalents of LiHMDS dropwise ...
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