- Preparation method of 5-chloro-2,2-dimethyl isobutyl valerate
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The invention relates to a preparation method of 5-chloro-2,2-dimethyl isobutyl valerate, which comprises the steps of carrying out heat exchange treatment and reaction on a phase A and a phase B, sequentially adding an isobutyl isobutyrate phase C, a 1,3-bromochloropropane phase D and a diluted hydrochloric acid phase E, reacting, quenching in a quenching module, and carrying out after-treatmentto obtain 5-chloro-2,2-dimethyl isobutyl valerate. According to the preparation method, metal lithium is replaced by n-butyllithium, so that the safety risk in the reaction process is reduced; a continuous flow micro-channel reactor is adopted, so that the reaction time is remarkably shortened, and the reaction efficiency is greatly improved; and the purity of the product reaches 97% or above, andthe yield reaches 91% or above.
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Paragraph 0100-0153
(2021/04/03)
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- Gemfibrozil derivatives as activators of soluble guanylyl cyclase – A structure-activity study
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Previous studies demonstrated that anti-hyperlipidemic drug gemfibrozil acts as NO- and heme-independent activator of NO receptor soluble guanylyl cyclase. A series of new gemfibrozil derivatives were synthesized and evaluated for sGC activation. The structure-activity relationship study identified the positions in gemfibrozil's scaffold that are detrimental for sGC activation and those that are amendable for optimizing modifications. Compared with gemfibrozil, compounds 7c and 15b were more potent activators of cGMP-forming activity of purified sGC and exhibited enhanced relaxation of preconstricted mouse thoracic aorta rings. These studies established the overall framework needed for futher improvement of sGC activators based on gemfibrozil scaffold.
- Baker, Hannah,Ferreira, Liam D.,Gayler, Kevin M.,Kane, Robert R.,Karunananthan, Johann W.,Kostyo, Jessica H.,Martin, Emil,Mattke, Jordan,Nguyen, Harold,Plunk, Michael A.,Quintana, Jeremy M.,Sharina, Iraida,Shuda, Mina,Stinchcomb, Alexandra L.
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- Preparation method of 5,5-dimethyl-2-cyanocyclopentanone
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The invention relates to a preparation method of 5,5-dimethyl-2-cyanocyclopentanone and a preparation method of a related intermediate 2,2-dimethyl-5-(4-chlorobenzyl)cyclopentanone and an application thereof to synthesis of a bactericide metconazole. Cholesteryl iso-butyrate, 1,3-dihalogenated propane, a cyanidation agent, p-chlorobenzyl chloride, and the like are used as main raw materials, multiple steps of reactions are used for preparation and separation, compared with a traditional process, the technique implementation is convenient and yield is high, and the methods have good industrial application prospects.
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Paragraph 0055; 0057
(2017/12/13)
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- Process for preparing 5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid
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An improved two-step process for preparing 5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid (gemfibrozil) which regularly affords gembibrozil in overall yields in excess of 80% comprises reacting an alkali metal salt of a lower alkyl ester of 2-methylpropanoic acid with 1,3-dibromopropane or 1-bromo-3-chloropropane in a polar aprotic solvent such as tetrahydrofuran, and then reacting the intermediate thus formed with an alkali metal salt of 2,5-dimethylphenol in a mixed toluene/dimethylsulfoxide solvent system.
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