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Novel process route for modified fatty acid type PET reagent precursor

A compound and selected technology are applied in the preparation of sulfonic acid esters, the preparation of carboxylic acid esters, and the preparation of carboxylic acids by oxidation, which can solve the problems of unfavorable industrial production of materials, excessively long synthesis routes, etc., and achieve low toxicity and danger of reagents, Simple to use effects

Active Publication Date: 2018-11-02
BEIJING SINOTAU INT PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its long synthetic route, the materials used are not conducive to industrial production

Method used

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  • Novel process route for modified fatty acid type PET reagent precursor
  • Novel process route for modified fatty acid type PET reagent precursor
  • Novel process route for modified fatty acid type PET reagent precursor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Reaction formula

[0106]

[0107] 1. Synthesis of Compound 1

[0108] Into a 1-liter three-neck flask, add magnesium chips and a little iodine, and replace and protect with nitrogen. Then 60 ml of anhydrous THF and a small amount of 6-bromo-1-hexene were added and the temperature was raised to initiate the reaction. After initiation, a solution of 162 g of 6-bromo-1-hexene in tetrahydrofuran was slowly added. After the dropwise addition, continue to stir until the reaction is complete.

[0109] Subsequently, 72 g of nonanal was added, and after the reaction was completed, the reaction was quenched with dilute hydrochloric acid, and extracted with dichloromethane. The organic phases were combined and desolvated and then purified by column chromatography. 68 g of compound 1 was obtained as a pale yellow liquid with a yield of 77%.

[0110] 1 H-NMR (300MHz, CDCl 3 )δ: 0.88(t, 3H), 1.28-1.47(m, 20H), 2.06(m, 2H), 3.58(m, 1H), 4.93(dd, 1H), 5.00(dd, 1H), 5.80(m ,...

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Abstract

The invention discloses a novel process route for a modified fatty acid type PET reagent precursor. The route has the characteristics of easily-obtained starting raw materials, simple route, mild reagent, high yield and the like.

Description

technical field [0001] The invention belongs to the field of organic chemical synthesis, and in particular relates to a new process route for modifying a fatty acid type PET reagent precursor. Background technique [0002] PET (Positron Emission Computed Tomography) is a relatively advanced clinical examination imaging technology in the field of nuclear medicine. The general method is to label a certain substance, generally a necessary substance in the metabolism of biological life, such as glucose, protein, nucleic acid, fatty acid, with a short-lived radionuclide (such as F 18 , C 11 etc.), after injected into the human body, through the accumulation of the substance in the metabolism, to reflect the situation of life metabolic activities, so as to achieve the purpose of diagnosis. [0003] In the basic aerobic metabolism of the myocardium, 70% of ATP is produced by β-oxidation of fatty acids, so fatty acids or modified fatty acids are suitable cardiac positron emission ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C303/28C07C309/66
CPCC07C29/38C07C41/01C07C45/00C07C45/41C07C51/16C07C67/08C07C67/26C07C67/31C07C303/28C07D301/14C07D303/22C07C309/66C07C69/675C07C69/708C07C59/13C07C47/198C07C43/162C07C47/37C07C69/757C07C43/15C07C33/025Y02P20/55
Inventor 徐新盛刘爽
Owner BEIJING SINOTAU INT PHARMA TECH CO LTD