37 results about "2-chloropyrimidine" patented technology

The invention relates to a synthetic method of an anti-tumor medicine, namely N-[2-[[2-(dimethylamino) ethyl] methyl amino]-4-methoxy-5-[[4-(1-methyl-1H-indole-3-yl)-2-pyrimidyl] amino] phenyl]-2-acrylamide (AZD9291) and a key intermediate of the anti-tumor medicine. The synthetic method comprises the following steps: performing Boc acid anhydride protection on 4-fluoro-2-methoxy-5-nitroaniline to obtain 4-fluoro-2-methoxy-5-nitroanilino tert-butyl formate, then reacting with N,N,N'-trimethylethylenediamine to obtain 4-(N,N,N'-trimethylethylenediamino)-2-methoxy-5-nitroanilino tert-butyl formate, then reducing to obtain 2-(N,N,N'-trimethylethylenediamino)-4-methoxy-5-tert-butyl carbamate phenylamine, then completely reacting with acryloyl chloride and directly removing a Boc protecting group to obtain 2-methoxy-4-N,N,N'-trimethylethylenediamino-5-acrylamido phenylamine, and finally reacting with 3-(2-chloropyrimidine-4-yl)-1-methylindole to obtain AZD9291. A process disclosed by the invention is simple in step, relatively high in yield, mild in reaction condition and easy for realization of industrial production.

The invention discloses a method for synthesizing 2,2'-dindolylmethane compounds. Firstly, 1-(pyrimidinyl-2-yl)-1H-indole compounds are generated in the mode that indole or substituded indole reacts with 2-chloropyrimidine under the sodium hydride alkaline condition with indole compounds as raw materials, indole guiding groups are introduced into the indole compounds, then the 1-(pyrimidinyl-2-base)-1H-indole compounds are subjected to a dimerization reaction under the action of acetic acid copper, silver nitrate and a toluene solvent, and finally the 2,2'-dindolylmethane compounds are synthesized. A direct carbon activation reaction method is applied, reaction steps are reduced, economical efficiency of reaction is improved, the target product 2,2'-dindolylmethane compounds are efficiently synthesized under the mild condition, indole groups can be removed after the 2,2'-dindolylmethane compounds are de-protected, 2,2'-dindolylmethane is generated, and the structural unit has wide biological activity and application prospects.

The invention relates to a low-cost preparation method for palbociclib. The low-cost preparation method comprises the following steps: by taking 2,4-dichloro-5-cyanopyrimidine as an initial raw material, performing cyano Grignard and hydrolysis so as to obtain 5-acetyl-2,4-dichloropyrimidine, protecting carbonyl, performing amination, removing carbonyl, performing acylation reaction by using diketene and amino so as to obtain 5-acetyl-4-acetoacetamide-2-chloropyrimidine, performing intramolecular dehydration on the product so as to obtain 6-acetyl-8-cyclopentyl-5-methyl-2-chlorine-8H-pyridino-[2,3-d] pyrimidine-7-ketone, protecting 6 acetyl groups by using carbonyl, further realizing reaction with an aminopyridine derivative so as to obtain 4-{6-[(6-1,1 dialkoxyl) ethyl-8-cyclopentyl-5-methyl-7-keton-7,8 dihydropyridino-[2,3-d]pyrimidine-2-amino]-pyridine-3-yl}-piperazine-1-carboxylic acid tert-butyl ester, and finally performing acid hydrolysis and neutralization to obtain palbociclib free alkali. By adopting the low-cost preparation method, the raw materials are easy to obtain, the cost is low, and the environment can be protected.