32779-36-5Relevant articles and documents
Preparation method 2 - methyl -5 -bromopyrimidine
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Paragraph 0034-0036, (2021/11/26)
The invention specifically discloses a preparation method of 2 - methyl -5 -bromopyrimidine, and belongs to the technical field of organic synthesis. The method comprises the following steps: a) taking 2 - amino -5 -bromopyrimidine as a raw material, carrying out diazotization reaction or Schedman reaction or 2 - hydroxyl -5 -bromopyrimidine as a raw material to obtain 2 -halo -5 -bromopyrimidine through a halogenated reagent. b) The carboxylic diester is substituted with 2 - halo -5 - bromopyrimidine to give 2-position substituted product. c) The last 2 -bit substituted product is reacted under basic, high temperature conditions to give 2 - methyl -5 - bromopyrimidine. The method has the advantages of easily available raw materials, low cost, simple flow and potential industrial amplification prospect.
Preparation method for 2-chloro-5-(piperidin-4-yl)pyrimidine
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Paragraph 0020; 0021; 0022, (2018/04/02)
The invention discloses a preparation method for 2-chloro-5-(piperidin-4-yl)pyrimidine. The target product is obtained by using 2-chloropyrimidine as a starting raw material, performing a brominationreaction, performing a coupling reaction, performing an elimination reaction and performing a catalytic hydrogenation reaction. The compound provided by the invention is an important pharmaceutical intermediate.
Preparation of 2-amino-pyrimidine-5-boronic acid frequency that ester method
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Paragraph 0017, (2017/01/02)
A method of preparing 2-aminopyrimidine-5-boronic acid pinacol ester is disclosed. The method includes subjecting 2-chloropyrimidine that is a raw material and NBS to bromization under catalysis of BF3-Et2O to obtain 2-chloro-5-bromopyrimidine; reacting the 2-chloro-5-bromopyrimidine with n-Bu3MgLi at a temperature ranging from -20 DEG C to -10 DEG C; adding methoxyboronic acid pinacol ester or isopropoxyboronic acid pinacol ester; performing boronization to obtain 2-chloropyrimidine-5-boronic acid pinacol ester; adding into ammonia water or a methanol-ammonia solution; and reacting at 80-100 DEG C in a sealed manner to obtain the 2-chloropyrimidine-5-boronic acid pinacol ester. Synthetic process conditions of the method are mild. An ultralow-temperature reaction is avoided. Reactions can be performed continuously. A pure product can be obtained only by simple recrystallization of the final product.