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A kind of synthetic method of 2,5-dihydroxyvaleric acid delta lactone

A technology of hydroxyvaleric acid and synthesis method, applied in directions such as organic chemistry, can solve problems such as tediousness, high cost and low yield, and achieve the effects of simple operation, low cost and high yield

Inactive Publication Date: 2016-04-27
NANJING PHARMATECHS
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Problems solved by technology

The traditional synthetic route of intermediates has cumbersome conditions, high cost and low yield

Method used

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  • A kind of synthetic method of 2,5-dihydroxyvaleric acid delta lactone

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Embodiment 1

0.016

[0016] 2). Operation:

[0017] Prepare a 250ml dry three-neck flask, add Hcc095-1 and phosphorus tribromide under nitrogen protection, heat to 100°C, add bromine dropwise within 2h15 minutes, the process is exothermic, after the addition, the temperature is raised to 120°C, heat preservation reaction for 2.5 h, stop heating and cool down, depressurize and spin off excess bromine to obtain a black viscous oil, which is directly cast into the next step.

[0018] 2. Synthesis of Hcc095:

[0019] substance Molar molecular weight (g / mol) Feeding amount (g) Amount of substance (mol) Volume (ml) The molar ratio of Hcc095-2 181 39.82 0.22

1 CaCO 3 100 20 0.2

0.91 h 2 o

240

[0020] 2). Operation:

[0021] Add the Hcc095-2 obtained in the previous step into a 500ml single-necked bottle, slowly add water while stirring, and add CaCO in batches 3 , After adding, heat to reflux overnight. The next d...

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Abstract

The invention aims to provide a synthesizing method of 2,5-dihydroxyvaleric acid delta lactone. The synthesizing method comprises an improved and economical method for synthesizing lactone derivatives and the like. Importantly, the synthesizing method is suitable for high-selectivity low-cost mass production.

Description

technical field [0001] The invention belongs to the field of chemical synthesis, and in particular relates to a synthesis method of 2,5-dihydroxyvaleric acid DELTA lactone. Background technique [0002] 2,5-dihydroxyvaleric acid deltalactone, English name 2,5-dihydroxyvalericaciddeltalactone, is a commonly used intermediate, mainly used in the synthesis of β-reductase inhibitor drugs, commonly used drugs are lovastatin, due to These drugs can effectively prevent the synthesis of endogenous cholesterol, so they can significantly reduce the level of cholesterol in the blood. The traditional synthetic route of intermediates has cumbersome conditions, high cost and low yield. Contents of the invention [0003] The object of the present invention is to provide a method for synthesizing 2,5-dihydroxypentanoic acid DELTA lactone, which includes an improved and more economical method for synthesizing lactone derivatives and analogues. Importantly, this method is applicable to la...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D309/30
Inventor 彭伟张晓文杨杰
Owner NANJING PHARMATECHS
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