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Preparation process of Alpelisib

A preparation process and t-bu technology, applied in the field of medicine, can solve the problems such as the preparation method of Alpelisib needs to be improved, and achieve the effects of small reaction difficulty, mild reaction conditions and fewer reaction steps.

Inactive Publication Date: 2020-04-07
武汉九州钰民医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] At present, the preparation method of Alpelisib still needs to be improved

Method used

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  • Preparation process of Alpelisib
  • Preparation process of Alpelisib
  • Preparation process of Alpelisib

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Embodiment Construction

[0045] Embodiments of the present invention are described in detail below. The embodiments described below are exemplary only for explaining the present invention and should not be construed as limiting the present invention. If no specific technique or condition is indicated in the examples, it shall be carried out according to the technique or condition described in the literature in this field or according to the product specification. The reagents or instruments used were not indicated by the manufacturer, and they were all commercially available conventional products.

[0046] Synthesis of compound shown in embodiment 1 formula 2

[0047] At 0°C, under stirring, add the compound shown in formula 1 (11.4g, 0.1mol) and triethylamine (28.3g, 0.28mol) to dichloromethane (220mL) successively, and then keep stirring, at about 0°C Add slowly (Boc) 2 O (48.0 g, 0.25 mol), the temperature was raised to 35-40°C and the reaction was stirred for 2 hours. Add 10% citric acid solut...

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Abstract

The invention relates to a preparation process of Alpelisib. The preparation process has the advantages of few reaction steps, simple process, mild reaction conditions, no extreme low-temperature reaction, simple purifying and low overall reaction difficulty, and is suitable for large-scale production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation process of Alpelisib. Background technique [0002] Alpelisib (BYL719) was developed by Novartis, and the US FDA approved Novartis's Alpelisib tablets (specifications: 50mg, 150mg, 200mg) on ​​May 24, 2019. It is used in combination with fulvestrant for the treatment of hormone receptor positive (HR+) / human epidermal growth factor receptor 2 negative (HER2-) negative advanced metastatic breast cancer carrying PIK3CA mutations in men and postmenopausal women. Alpelisib is the first PI3K (specifically PI3Kα) inhibitor for the treatment of this type of breast cancer. [0003] Alpelisib is a selective phosphatidylinositol 3-kinase α (PI3Kα) inhibitor indicated for the treatment of patients with HR+ / HER2- advanced metastatic breast cancer carrying a PIK3CA mutation. Alpelisib's preclinical data show that the drug's inhibitory activity on PI3Kα is 50 times that of oth...

Claims

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Application Information

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IPC IPC(8): C07D417/14
CPCC07D417/14
Inventor 许勇陈龙顿伟余艳平范昭泽于静
Owner 武汉九州钰民医药科技有限公司
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