One is the synthesis method of ATP competitive small molecule AKT inhibitor A443654

A synthetic method and small molecule technology, applied in the production of bulk chemicals, organic chemistry, etc., can solve the problems of low total yield, unfriendly environment, high toxicity, etc., and achieve the effect of increased yield and shortened reaction time
CN104610229BActive Publication Date: 2017-01-18SHANGHAI HAOYUAN MEDCHEMEXPRESS CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI HAOYUAN MEDCHEMEXPRESS CO LTD
Publication Date
2017-01-18

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Abstract

The invention discloses a synthesis method of an ATP competitive small-molecule AKT inhibitor A443654. According to the method, a compound 1 is used as a starting raw material, and the compound 6 (A-443654) is obtained through amino group protection, Suzuki reaction and protecting group removal. Usage of poisonous reagent hexamethylditin is avoided, the method is high in safety, environment-friendly, high in reaction yield and suitable for industrial large-scale production, the reaction time is shortened, and the process cost is reduced. The flow chart of the synthesis method is shown in the specification.
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Description

[0001] Technical field:

[0002] The invention relates to a method for preparing a compound, in particular to a method for synthesizing ATP competitive small molecule AKT inhibitor A443654.

[0003] Background technique:

[0004] The PI3K / AKT / mTOR signaling pathway is an important signal transduction pathway in cells, which affects cell metabolism, proliferation, transcription, survival and angiogenesis, and is closely related to the occurrence and development of various tumors, and is also associated with diabetes, related to cardiovascular disease. AKT, also known as protein kinase B (protein kinase B, PKB), is a serine / threonine protein kinase. PI3K / AKT signaling is activated in normal tissues, and when the pathway is overactivated, the overexpression of p-AKT may lead to tumor cell death by down-regulating the tumor suppressor protein p53, stimulating protein synthesis, and inhibiting apoptosis. Unlimited value-added. Therefore, inhibiting the activation of this pathway ...

Claims

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