1231929-97-7Relevant articles and documents
A synthesis of abemaciclib utilizing a Leuckart-Wallach reaction
Frederick, Michael O.,Kjell, Douglas P.
, p. 949 - 951 (2015)
A concise total synthesis of CDK 4/6 inhibitor abemaciclib is described. The synthesis uses a Suzuki coupling, followed by a Hartwig-Buchwald amination to join three of the four subunits. The final step is a reductive amination utilizing Leuckart-Wallach conditions. Key to the Leuckart-Wallach reaction was the addition of trimethyl orthoformate to remove water formed during the reaction, allowing the reaction to go to completion.
Abecheli intermediate and simple preparation method of Abemaciclib
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, (2019/10/01)
The invention relates to an Abemaciclib intermediate and a simple preparation method of Abemaciclib. The Abemaciclib intermediate is 1-isopropyl-2-methyl-4-fluorine-6-(3-dimethylamino-2-fluorine) acryloyl-1H-benzimidazole (V), and also provides a preparation method of the Abemaciclib intermediate. The Abecheli intermediate and 5-(4-ethylpiperazine-1-yl) methyl-2-pyridylguanidine are subjected to pyrimidine cyclization reaction to prepare Abemaciclib (I). The method has the advantages of cheap and easily available raw materials, good stability of raw materials and intermediate products, mild reaction conditions, high reaction selectivity, high atom economy in the reaction process, high product purity and yield, low cost, less three wastes, environmental protection and contribution to the industrial production of Abemaciclib.
PREPARATION METHOD FOR BEMACICLB
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, (2017/11/11)
Disclosed are an intermediate of bemaciclib or abemaciclib and a preparation method therefor. The preparation method comprises condensation, amidine reaction, cyclization and other unit reactions. Serving the intermediate of bemaciclib as a raw material, bemaciclib is obtained through the guanidination reaction and the cyclization reaction. According to the preparation method, the raw material is easily available, the procedure is simple, and the preparation method is economical, environmentally friendly and suitable for industrial production.