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Synthesis method of palbociclib intermediate

A synthesis method and Palbociclin technology, applied in the field of synthesizing Palbociclin intermediates, can solve the problems of complicated product obtaining process, inconvenient recovery, complicated product extraction and purification of hydrogenation reaction, etc., and achieve environmental protection improvement, product Yield and Purity Improvement, Product Yield and Purity Improvement Effect

Inactive Publication Date: 2018-09-21
苏州莱克施德药业有限公司
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Problems solved by technology

[0005] The advantage of this method is that there are few reaction by-products and high yield. The total yield of the two steps is 89%. The acquisition process is complicated, and the product extraction and purification of the hydrogenation reaction are complicated, and further optimization research is required

Method used

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  • Synthesis method of palbociclib intermediate
  • Synthesis method of palbociclib intermediate
  • Synthesis method of palbociclib intermediate

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Embodiment Construction

[0022] Synthesize the desired product through the following three steps, as follows:

[0023] 1, Synthesis of 2-nitro-5-bromopyridine (II)

[0024] Add 160ml of 30% hydrogen peroxide to a 1000ml three-necked reaction flask, use a low-temperature reaction bath to cool down to within 15°C, and use a constant pressure dropping funnel to drop 320ml of 98% concentrated sulfuric acid into the hydrogen peroxide in the reaction flask. The temperature of the solution in the bottle is controlled at 5 In the range of -15°C, solution B was obtained after the dropwise addition was completed. At the same time, add 160ml of 98% concentrated sulfuric acid to another 1000ml three-necked reaction flask, use a low-temperature reaction bath to cool down, add 60.00g of 2-amino-5-bromopyridine in batches, control the temperature within the range of 5-15°C, and obtain a solution after adding a.

[0025] Both solutions A and B have been prepared. Use a constant pressure dropping funnel to add solut...

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Abstract

The invention provides a synthesis method of a palbociclib intermediate, and particularly relates to the technical field of drug synthesis. The synthesis method comprises the process route of using 4-(6-aminopyridine-3-group)piperazine-1-tert-butyl formate and 2-amino-5-bromopyridine as raw materials, and obtaining a target product through oxidation, coupling and reduction. Factors influencing thereaction are subjected to systematical experiments and study. Compared with a traditional preparing technology, the process route is obviously improved in all the aspects of the production cost, thetechnological operation, the product yield and purity and the environment protection.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis, and in particular relates to a synthesis method of a palbocillin intermediate. Background technique [0002] Palbociclib is a novel oral cyclin-dependent kinase 4 / 6 (CDK4 / 6) inhibitor. It mainly plays a role by regulating the cell cycle, and prevents cells from G1 phase to S phase by inhibiting CDK4 / 6 activity, thereby inhibiting DNA synthesis. Developed by Pfizer of the United States, it was approved by the FDA for marketing in the United States on February 3, 2015 through an accelerated approval route. It is clinically used in combination with letrozole for the treatment of postmenopausal estrogen receptor (ER) positive, human epidermis Initial endocrine therapy for metastatic disease in patients with growth factor receptor 2 (HER2)-negative advanced breast cancer. The Palbociclib phase III trial PALOMA-3 study added palbociclib to the standard fulvestrant regimen to treat previous...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/75C07D213/61
CPCC07D213/61C07D213/75
Inventor 汪爱丰刘传涛张彩慧俞菊荣
Owner 苏州莱克施德药业有限公司
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