952518-97-7Relevant articles and documents
Preparation of 4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidine
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Paragraph 0023; 0028-0029, (2021/11/03)
The invention relates to a preparation method of 4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin. Specifically, 1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidine acetonitrile is subjected to a chemical reaction under the action of acid, so the preparation of the 4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidine is realized.
Preparation method of key intermediate 2 for synthesizing baricitinib
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Paragraph 0084; 0085; 0100; 0111; 0112, (2018/04/28)
The invention relates to a preparation method of a key intermediate 2 for synthesizing baricitinib. The preparation method comprises the following process steps: respectively synthesizing an intermediate A, an intermediate B, an intermediate D and the key intermediate 2. The preparation method has the advantages that commercially available raw materials, i.e. 1H-pyrazole-4-formic acid (SM1), ethylcyanoacetate (SM2), 2-bromo-1,1-diethoxyethane (SM3) and formamidine acetate ( SM4) are used as starting materials, and the key intermediate 2 is obtained after only four steps of chemical reactionsare carried out; the use of starting materials such as 4-chloropyrrolo[2,3-d]pyrimidine and pyrazol borate which are high in material cost is avoided, and the production cost of the key intermediate 2is lowered.