Dipeptide boric acid composed of carboxylic acid and alpha-amino acid as well as ester compound thereof, and preparation method and application of dipeptide boric acid and ester compound thereof

A technology of ester compounds and peptide boronic acid, which is applied in the field of preparation of new peptide boronic acid and its ester compounds, can solve the problems of patients with heavy economic burden, diarrhea and neuropathy

Active Publication Date: 2016-07-06
JIANGSU CHIA TAI FENGHAI PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The price of Velcade in the Chinese market is about 13,000 yuan per 3.5 mg, and the cost of one cycle of treatment is about 40,000 yuan. Such an expensive cost is a very h

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  • Dipeptide boric acid composed of carboxylic acid and alpha-amino acid as well as ester compound thereof, and preparation method and application of dipeptide boric acid and ester compound thereof
  • Dipeptide boric acid composed of carboxylic acid and alpha-amino acid as well as ester compound thereof, and preparation method and application of dipeptide boric acid and ester compound thereof
  • Dipeptide boric acid composed of carboxylic acid and alpha-amino acid as well as ester compound thereof, and preparation method and application of dipeptide boric acid and ester compound thereof

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Embodiment Construction

[0058] Synthesis of the first part of the compound

[0059] The preparation of the compound of the present invention can be carried out according to the following process:

[0060] One, the preparation of compound (II)

[0061]

[0062] 1. Preparation of N-ethyl acetate phthalimide II-1:

[0063] Dissolve phthalimide in DMF, add triethylamine, add ethyl chloroacetate dropwise to the reaction system at 0°C, slowly rise to room temperature and react for 2 hours, pour the reaction solution into ice water, filter , the filter cake was washed with ice water, and vacuum-dried to obtain the pure compound (formula II-1).

[0064] 2. Preparation of N-phthaloyl-protected alanine II-2:

[0065] Compound II-1 and L-alanine were dissolved in H 2 O, add Na 2 CO 3 After reacting for 2 hours, add 1N HCl to adjust the pH value to 2, filter, and dry in vacuum to obtain the pure compound (formula II-2).

[0066] 3. Preparation of compound II-3:

[0067] Compound II-2 was dissolved in ...

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Abstract

The invention belongs to the field of drug synthesis and in particular relates to a series of novel peptide boric acids as well as an ester compound or pharmaceutical salt thereof, and a preparation method and application of the peptide boric acids as well as the ester compound or pharmaceutical salt thereof in pharmacodynamics. A structure of the peptide boric acid and the ester compound or pharmaceutical salt thereof is shown in a formula I (described in the specification). The compound provided by the invention can be used for preparing a proteasome inhibitor and can further be used for treating solid tumours and blood tumours, wherein the solid tumours are selected from non-small cell lung cancer, small cell lung cancer, lung adenocarcinoma, lung squamous carcinoma, pancreatic cancer, breast cancer, prostate cancer, liver cancer, skin cancer, epithelial cell cancer, gastrointestinal stromal tumor, nasopharynx cancer and leukemia; and the blood tumours are selected from multiple myeloma, mantle cell lymphoma and histiocytic lymphoma.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a series of preparation methods of novel peptide boronic acid and its ester compounds and their application in pharmacodynamics. Background technique [0002] At present, cancer is one of the most important diseases that endanger human health. Although the current treatment of cancer has made great progress in the fields of surgical treatment, chemotherapy, and radiotherapy, it still cannot fundamentally treat cancer. Although the currently marketed anticancer drugs have certain curative effects, they have serious toxic and side effects. Therefore, in-depth exploration and research on how to start from effective tumor targets to study targeted new anticancer drugs has become a top priority for medical workers. [0003] The Ubiquitin-Proteasome Pathway (UPP) is the main pathway for the degradation of intracellular protein systems and is involved in many physiologically ...

Claims

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Application Information

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IPC IPC(8): C07F5/02A61K31/69A61P35/00A61P35/02
CPCC07F5/025
Inventor 雷萌朱永强冯华云王成
Owner JIANGSU CHIA TAI FENGHAI PHARMA
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