78712-80-8Relevant articles and documents
Synthesis method of beta-chloro acid ester and alpha, beta-unsaturated acid ester compound
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Paragraph 0138-0142, (2021/08/11)
The invention belongs to the technical field of organic chemistry, and particularly relates to a synthesis method of beta-chloro acid ester and an alpha, beta-unsaturated acid ester compound. The structure of the compound is characterized by 1H NMR and 13C NMR and is confirmed. The method comprises the steps of by taking acetonitrile as a solvent, carrying out fragmentation on olefin, chlorooxalic acid monoester and 2, 6-dimethyl pyridine under a photocatalytic condition to generate an alkoxyacyl free radical intermediate, carrying out free radical addition reaction on the alkoxyacyl free radical intermediate and the olefin to generate carbon free radicals, then carrying out chlorination reaction to obtain the beta-chloro acid ester compound, and carrying out dehydrochlorination reaction under a DBU condition to generate the alpha, beta-unsaturated acid ester compound. The preparation method of the compound disclosed by the invention has the advantages of starting from olefin, being mild in condition, simple and efficient, strong in functional group compatibility and wide in substrate application range, and various beta-chloro acid ester and alpha, beta-unsaturated acid ester compounds can be synthesized from highly commercialized raw materials. On the basis of photoreaction of fluid chemistry, a target product can also be obtained with a relatively good yield, and the method has very good industrial and medicinal chemistry application values.
Synthesis method of ozagrel sodium
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Paragraph 0045-0047, (2020/07/12)
The invention discloses a synthesis method of ozagrel sodium, and belongs to the technical field of medicines. The synthesis method comprises the following steps: (1), taking 4-bromobenzyl bromide asa starting material, and reacting with imidazole under an alkaline condition to generate a 1-(4-bromobenzyl)-1H-imidazole intermediate 1; (2), enabling 1-(4-bromobenzyl)-1H-imidazole to react with acrylate under the catalysis of palladium acetate to generate an ozagrel ester intermediate 2; and (3), carrying out alkaline hydrolysis on ozagrel ester to obtain an ozagrel sodium product. The synthesis method disclosed by the invention has the advantages of easily available raw materials, low price cost, few steps, small pollution and the like, and is suitable for industrial production.
Highly selective inhibitors of thromboxane synthetase. 1. Imidazole derivatives
Iizuka,Akahane,Momose,Nakazawa,Tanouchi,Kawamura,Ohyama,Kajiwara,Iguchi,Okada,Taniguchi,Miyamoto,Hayashi
, p. 1139 - 1148 (2007/10/02)
The structure-activity relationships of imidazole derivatives as inhibitors of thromboxane (TX) synthetase were investigated. Introduction of various substituents (e.g., one or two methyl groups, a halogen atom, a methylidene group, unsaturated bonds, or a phenylene group) into the α position or other positions in the carboxy-bearing side chain of 1-(7-carboxyheptyl)imidazole was found to increase the inhibitory potency. The length of the side chains with the phenylene group was optimum for the inhibitory potency on TX synthetase in the region of 8.5-9.0 A. Among the tested imidazole derivatives, 1-(7-carboxy-7-methyl-2-octynyl)imidazole, 4-[3-(1-imidazolyl)-propyl]benzoic acid, and (E)-4-(1-imidazolylmethyl)cinnamic acid and its α-methyl analogue showed the highest potency with an IC50 in the range of 10-8 to 10-9 M. Inhibition by these derivatives was highly selective for the TX synthetase, since other enzymes such as fatty acid cyclo-oxygenase and prostacyclin synthetase were not affected.
