7340-22-9Relevant academic research and scientific papers
Preparation method of 2-pyridylacrylic acid
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Paragraph 0012; 0015-0022, (2020/02/19)
The invention belongs to the field of organic synthesis, and in particular, relates to a preparation method of 2-pyridylacrylic acid. The method comprises the following steps: by taking 2-pyridylaldehyde as a raw material and pyridine as a solvent, adding malonic acid, adding a catalyst after complete dissolution, heating to 60-70 DEG C, carrying out a reaction for 2.5-3 h, performing thin-layer chromatography tracking reaction, after the reaction is completed, cooling the reaction liquid to 0-5 DEG C, then pouring into an ice-water mixture of concentrated hydrochloric acid, separating out solids, and carrying out suction filtration to obtain the required product 2-pyridylacrylic acid. The method has the beneficial effects that the reaction conditions are mild, the operation is easy, the post-treatment is simple, the scale-up production is easy, and the method is quite suitable for industrial production; the catalytic effect is good, and the yield is high; the raw materials are cheap and the production cost is low.
Radical-Cation Vinylcyclopropane Rearrangements by TiO2Photocatalysis
Maeta, Naoya,Kamiya, Hidehiro,Okada, Yohei
supporting information, p. 6551 - 6566 (2020/07/14)
Radical cation vinylcyclopropane rearrangements by TiO2 photocatalysis in lithium perchlorate/nitromethane solution are described. The reactions are triggered by oxidative single electron transfer, which is followed by immediate ring-opening of the cyclopropanes to generate distonic radical cations as unique reactive intermediates. This approach can also be applied to vinylcyclobutane, leading to the construction of six-membered rings. A stepwise mechanism via distonic radical cations is proposed based on preliminary mechanistic studies, which is supported by density functional theory calculations.
Preparation method of 2-pyridine acrylic acid
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Paragraph 0015-0022, (2019/05/28)
The invention belongs to the field of organic synthesis, and particularly relates to a preparation method of 2-pyridine acrylic acid. The method includes following steps: taking 2-pyridylaldehyde as araw material and pyridine as a solvent, adding malonic acid, adding a catalyst after complete dissolution, rising temperature to 60-70 DEG C, allowing reaction for 2.5-3h, allowing thin-layer chromatography tracking reaction, cooling reaction liquid to 0-5 DEG C after reaction is completed, pouring the reaction liquid into an ice-water mixture of concentrated hydrochloric acid, separating out solid, and performing suction filtering to obtain 2-pyridine acrylic acid. The method has the advantages of being mild in reaction condition, easy in operation, simple in aftertreatment, easy in amplifying production, quite suitable for industrial production, good in catalytic effect, high in yield, low in raw material cost and low in production cost.
Isocytosine H2-receptor histamine antagonists II. Synthesis and evaluation of biological activity at histamine H1- and H2-receptors of 5-(heterocyclyl)methylisocytosines
Brown, Thomas H.,Blakemore, Robert C.,Blurton, Peter,Durant, Graham J.,Ganellin, C. Robin,et al.
, p. 65 - 72 (2007/10/02)
A series of 2--4-pyrimidones was synthesized based on oxmetidine 2, in which the methylenedioxyphenyl group of 2 was replaced by a heterocyclic ring.Good H2-receptor antagonist activity was retained over a range of basic and neutral heterocyclic substituents.Replacement of the 5-methyl-4-imidazolyl ring in selected compounds with 2-thiazolyl and, particularly, 3-bromo-2-pyridyl rings gave a series of compounds which have both H1- and H2-receptor histamine antagonist activities.Some structure-activity and structure-toxicity correlations are discussed.Compound 6d, 2--5-(6-methylpyrid-3-yl)-4-pyrimidone, has the most favourable combination of properties for H2-antagonism and has been evaluated further as an anti-secretory agent.
