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Magnetic resonance imaging compound, magnetic resonance imaging agent and application thereof as well as magnetic resonance imaging method

A technology of nuclear magnetic resonance and compounds, applied in the direction of pharmaceutical formulations, preparations for in vivo tests, peptides, etc., to achieve the effect of enhancing contrast

Active Publication Date: 2018-02-06
BEIJING NEUROSURGICAL INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this type of benzamidomethylpyrrolidine NMR imaging compound cannot penetrate the cell membrane and enter the nucleus for imaging

Method used

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  • Magnetic resonance imaging compound, magnetic resonance imaging agent and application thereof as well as magnetic resonance imaging method
  • Magnetic resonance imaging compound, magnetic resonance imaging agent and application thereof as well as magnetic resonance imaging method
  • Magnetic resonance imaging compound, magnetic resonance imaging agent and application thereof as well as magnetic resonance imaging method

Examples

Experimental program
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preparation example Construction

[0080] The preparation method used in the specific embodiment:

[0081] 1. Washing general method. The following "washing" of the solid phase resin refers to washing the resin three times alternately with DMF × 2 times, DCM × 2 times, DMF × 2 times after filtering out the reaction solution, each time for 2 to 3 minutes.

[0082] 2. Condensation method. The general method for the condensation of solid phase resins is as follows: 3 times excess of protected amino acids, 3 times of excess condensing agent (HCTU unless otherwise specified), and 3 times of excess Cl-HOBt are dissolved in an appropriate amount of DMF to obtain 0.25mmol / ml solution, add a 6-fold excess DIPEA to the solution, stir for 1 minute, then add it to the N-terminal deprotected resin, shake and mix at room temperature for 2 hours and wash according to the "washing method".

[0083] 3. Deprotection general method. The general method for removing the N-Fmoc protecting group from the solid-phase resin is as fo...

preparation example 1

[0088] Preparation Example 1. Preparation of N-tert-butoxycarbonyl (O-benzyl) seryl diethylamide (1a)

[0089]

[0090] 11.814g (40mmol) N-tert-butoxycarbonyl (O-benzyl) serine Boc-Ser(Bzl)-OH, 5.06g N-hydroxysuccinimide (HOSu) and 6.715g dicyclohexylcarbodiimide (DCC) was dissolved in 100ml of anhydrous DCM, DIPEA was added under an external ice water bath and stirred for 30 minutes, then returned to room temperature and stirred for 8 hours, and the reaction solution was filtered with 1mol / L hydrochloric acid, saturated NaHCO 3 aqueous solution and saturated NaCl aqueous solution were washed three times each, and the organic layer was washed with NaCl 2 SO 4 After drying and filtering, the filtrate was concentrated and dried in a vacuum oven at 45°C. Dissolve the obtained product in 200ml of anhydrous DCM, drop into 18.4ml of ethylenediamine solution, and stir in an external ice water bath for reaction. Remove the ice bath after dripping. React at room temperature for 4 ...

preparation example 2

[0092] Preparation example 2. Preparation of (O-benzyl) seryl diethylamine hydrochloride (1b)

[0093]

[0094] Add 10ml of methanol to 9.418g (27.9mmol) of compound 1a prepared in Preparation Example 1, add 3mol / L saturated HCl ethyl acetate solution, stir the reaction in an external ice water bath for 3 hours, concentrate the reaction solution, and dry it in a vacuum oven at 45°C After 12 hours, 8.118 g of a light yellow solid was obtained, with a yield of 93.7%.

[0095] Product Analysis: ESI-MS: Calculated 238.15 [M+H]+, found: 238.15.

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Abstract

The invention relates to a stapled peptide type compound or pharmaceutically acceptable salt thereof, a magnetic resonance imaging agent and application thereof as well as a magnetic resonance imagingmethod. The stapled peptide type compound has a general formula structure shown in a formula (I), wherein R1, R2, R3, Ln and Xaa are defined in the specification. The stapled peptide type magnetic resonance imaging compound can penetrate a cell membrane, and enter a cell nucleus to be combined with an estrogen receptor located in the cell nucleus, and intracellular imaging is carried out specifically and selectively in a targeting manner. (The formula (I) is described in the specification).

Description

technical field [0001] The invention relates to a nuclear magnetic resonance imaging compound, a nuclear magnetic resonance imaging agent and application, and a nuclear magnetic resonance imaging method. Background technique [0002] Estrogen can regulate various physiological processes such as growth, replication, development, and differentiation of normal tissues and cells, and is also involved in the occurrence and development of various tumors. Estrogen acts on cells mainly through the two ER subtypes of estrogen receptor (ER) α and β. Abnormal estrogen signal transduction can promote the occurrence and development of various tumors. Estrogen and estrogen receptors are important factors affecting the biological behavior of various hormone-sensitive tumors such as breast cancer, endometrial cancer, and pituitary adenoma, and are important drug targets for various tumors. Pituitary adenomas account for 10-15% of all brain tumors and are the second largest intracranial tu...

Claims

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Application Information

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IPC IPC(8): C07K7/08A61K49/14
CPCA61K49/14C07K7/08
Inventor 刘潜张亚卓杨潇骁高华李储忠
Owner BEIJING NEUROSURGICAL INST
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