5034-74-2Relevant academic research and scientific papers
Stereocontrolled Formal Synthesis of Platencin
Hsu, Day-Shin,Hwang, Tai-Yu
, p. 4689 - 4695 (2018)
A stereocontrolled formal synthesis of platencin was accomplished in 11 steps from a bromophenol derivative, with an overall yield of 13 %. The intermolecular Diels–Alder reaction of masked o-benzoquinone and an aldol condensation were the key steps in th
Formal total synthesis of salvianolic acid N
Wu, Kong,Xie, Zhong Pao,Cui, Dong-Mei,Zhang, Chen
, p. 832 - 837 (2018)
An efficient synthetic pathway for the total synthesis of salvianolic acid N has been reported. The key reaction steps, the Wittig reaction for Z-stereoselectivity and an intramolecular cyclization for a seven membered ring skeleton, have been optimized to improve the synthetic feasibility and provide the best conditions in terms of yield. Moreover, a notable reaction is the reaction of the deprotected allylic group with Pd catalyst. An improved overall yield of 11% has been achieved for salvianolic acid N starting from 3,4-dimethoxybenzaldehyde in 11 steps.
Substituent Effects and Mechanism in a Mechanochemical Reaction
Barbee, Meredith H.,Kouznetsova, Tatiana,Barrett, Scott L.,Gossweiler, Gregory R.,Lin, Yangju,Rastogi, Shiva K.,Brittain, William J.,Craig, Stephen L.
, p. 12746 - 12750 (2018)
We report the effect of substituents on the force-induced reactivity of a spiropyran mechanophore. Using single molecule force spectroscopy, force-rate behavior was determined for a series of spiropyran derivatives substituted with H, Br, or NO2/sub
TETRAHYDROISOQUINOLINE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF
-
Paragraph 0352-0354, (2021/09/10)
Provided are a tetrahydroisoquinoline derivative, a preparation method therefor and an application thereof in medicine. In particular, provided are a tetrahydroisoquinoline derivative represented by general formula (I), a preparation method therefor and a
Synthetic method 5 - bromo -1 and 2,3 - trimethoxy benzene
-
Paragraph 0038-0040; 0045-0054, (2021/10/30)
The synthesis method of 5 -bromo -1-2,3 -methoxy benzene comprises the following steps: S1, taking the vanillin as a starting raw material, and brominating 5 - bromo -2 - hydroxyl -3 -methoxybenzaldehyde through the hydroxyl group para-position. S2 is obt
Synthesis method 5 - halogeno-veratraldehyde
-
, (2021/11/21)
The invention belongs to the field of organic chemistry, and in particular relates 5 - to a method for synthesizing halogenated O-veratraldehyde by using 4 - halogenoylguaiacol as a raw material to obtain 2 -hydroxy -3 - methoxy -5 -halogenated mandelic a
A synthetic preparation method for small carbags hydrochloric acid
-
, (2021/12/08)
The present invention belongs to the field of organic chemistry, relates to a method of synthesizing berberine hydrochloride, comprising: S1: with 5-halo-o-quinoastearaldehyde and piperine ethylamine to obtain N- [2-(3,4-dimethoxyphenyl-5-yl) ethyl] -1- (5-halo-2,3-dimethoxybenzyl) methylimide; S2: to obtain 2- (3,4-diimoxyphenyl) -N- (5-bromo-2,3-dimethoxybenzyl) ethylamine; S3: to obtain 2-(3,4-dimethoxyphenyl) -N- (5-bromo-2 S4: to obtain 12-halogenated berberine derivative; S5: to obtain berberine. The present invention is free from the application of the by-product o-vanillin synthesis of o-resveratal raw material constraints, synthesis of 5- substitute o-resveratal and piperine ethylamine, and the use of the two preparation of berberine hydrochloride, with raw materials readily available, mild reaction conditions, easy to operate, high chemical yield, low cost and other advantages.
Synthesis and assessment of 3-substituted phenazines as novel antich-lamydial agents
Bao, Xiaofeng,Liu, Ziyi,Ni, Min,Xia, Chao,Xu, Shunxin,Yang, Shengju,Zhao, Yu
, p. 413 - 421 (2020/04/17)
Background: In the past century, many phenazines were isolated from the marine mi-croorganism, and some of these phenazines possessed potent antibacterial activities. We found that a few of the synthesized 4-substituted phenazines could block the infectivity of chlamydiae without host cell toxicity. Objective: The aim of this study was to design and synthesize two series of novel 3-substituted phenazines to find novel antichlamydial agents. Methods: The 3-substituted phenazines were synthesized via Buchwald-Hartwig cross coupling reaction and Suzuki reaction from 3-bromo-1-methoxyphenazine. The antichlamydial activity of these synthesized compounds was evaluated by determining their effect on the yield of infectious progeny EBs. Cytotoxicity of these compounds on host cells was assessed by the treatment of un-infected HeLa cells using WST-1 method. Results: Most of the 3-substituted phenazines possessed potent antichlamydial activity with IC50 values from 0.15 to 12.08 μM against Chlamydia trachomatis L2, C. muridarum MoPn and C. pneumoniae AR39. Among them, 7d and 9a exhibited better antichlamydial activity with IC50 values from 0.20 to 1.01 μM while they have no apparent cytotoxicity to host cells. Biological assay disclosed that both 7d and 9a inhibited chlamydial infection by reducing elementary body infectiv-ity and disturbing chlamydial growth during the whole chlamydial developmental cycle. Conclusion: Our findings suggested that 3-substituted phenazine derivatives might be a promising class of therapeutic agents for chlamydial infections. More effective phenazines with low toxicity could be acquired through further chemical modification on C-3 position rather than C-4 position of phenazine.
Imidazo ring PAR4 antagonist and medical applications thereof
-
Paragraph 0432-0435, (2020/01/12)
The invention relates to an imidazo ring compound represented by formula (I) or formula (II), or a pharmaceutically acceptable salt or ester or solvate thereof. The compound disclosed by the inventioncan be used for preparing medicines for preventing or treating thromboembolic diseases.
Synthesis of Benzodioxane and Benzofuran Scaffolds Found in Neolignans via TMS Triflate Mediated Addition to 1,4-Benzodioxane Hemiacetals
Jung, Eun-Kyung,Pilkington, Lisa I.,Barker, David
, p. 1190 - 1205 (2017/03/11)
This research reports the successful asymmetric synthesis of both a 9-hydroxy-5′-methoxy-1,4-benzodioxane framework and a highly functionalised benzofuran scaffold. Both synthetically desirable structures are the result of a Lewis acid catalysed addition
