7150-01-8Relevant academic research and scientific papers
Overcoming AlbD Protease Resistance and Improving Potency: Synthesis and Bioactivity of Antibacterial Albicidin Analogues with Amide Bond Isosteres
Kleebauer, Leonardo,Zborovsky, Lieby,Hommernick, Kay,Seidel, Maria,Weston, John B.,Süssmuth, Roderich D.
supporting information, p. 7023 - 7027 (2021/09/08)
Albicidin is a potent antibacterial oligoaromatic peptide that is susceptible to the protease AlbD, a resistance factor. This potentially restricts the use of albicidin as a drug. To overcome this obstacle, we synthesized and evaluated six analogues with
Boron Containing PDE4 Inhibitors
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Paragraph 0635-0636, (2020/04/29)
The present invention relates to boron containing compounds of Formula (I) [in-line-formulae]X—Y—Z?? Formula (I)[/in-line-formulae] that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
The first total synthesis of (±)-methyl salvianolate A using a convergent strategy
Wang, Bo,Wang, Liping,Peng, Ying,Pang, Yiying,Xiao, Hesheng,Wang, Xiaoji,Huang, Shuangping
, (2019/03/19)
Herein, a convergent, practicable and first total synthesis of the natural product, (±)-methyl salvianolate A, is reported. The key features of the approach are the use of a Horner–Wadsworth–Emmons reaction and the protection of multiple hydroxyls using s
COMPOUNDS FOR TREATMENT OF CARDIAC ARRHYTHMIAS AND HEART FAILURE
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Page/Page column 55, (2019/10/19)
This disclosure concerns compounds and a method for modulating the activity of calcium ion channels, including Ca2+-induced (or Ca2+-activated) calcium release channels and conformationally coupled calcium release channels such as ryanodine receptors. Some of the compounds have a structure according to formula I, or a stereoisomer, tautomer, hydrate, solvate, prodrug, or pharmaceutically acceptable salt thereof.
Salvianolic acid A intermediate and preparation method thereof
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Paragraph 0074; 0075; 0092; 0093; 0101; 0102; 0110; 0111, (2018/09/08)
The invention relates to a medicine salvianolic acid A intermediate used for treating angina and acute myocardial infarction, i.e., a new synthesis method for trans-3-bromo-2-(3,4-di-substituted styryl)-6-substituted phenol. The method comprises the follo
Fibrauretine synthetic method (by machine translation)
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Paragraph 0042; 0043; 0061, (2018/09/21)
The invention relates to O-vanillin (11) as the starting material, by the acylation reaction generating 2 - acetoxy - 3 - methoxybenzaldehyde (12), by the bromo, hydrolysis reaction to produce the 2 - hydroxy - 6 - bromo - 3 - methoxybenzaldehyde (13), produced by the methylation reaction 6 - bromo - 2, 3 - dimethoxy benzaldehyde (14), produced by the condensation reaction of 2 - (6 - bromo - 2, 3 - dimethoxyphenyl) - 1, 3 - dioxolane (15); and then to 3, 4 - dimethoxy acetic acid (21) as raw materials, generated by the reduction reaction of the 3, 4 - dimethoxy ethanol (22), the acylation reaction generated by 3, 4 - dimethoxy new valeric acid environmentally (23), the acylation reaction is generated by the 2 - ethoxy - 3, 4 - dimethoxy new valeric acid environmentally (24), intermediate (15) and (24) after coupling, cyclized two-step reaction process for preparing the target product fibrauretin. (by machine translation)
Synthesis of (+)-salvianolic acid A from sodium Danshensu
Xu, Kai,Liu, Hao,Liu, Delong,Sheng, Cheng,Shen, Jiefeng,Zhang, Wanbin
, p. 5996 - 6002 (2018/09/06)
(+)-Salvianolic acid A, one of the most active components in the traditional Chinese medicine Danshen, has been synthesized over 10 steps in 6.5% overall yield. Starting from inexpensive ortho-vanillin and sodium Danshensu (synthesized via asymmetric catalysis in our group), the process consists of the following: A Wittig reaction that gives the desire product with absolute E-configuration, a demethylation reaction with AlCl3 in a satisfactory yield, and a practical deprotection of allylic groups to afford the terminal product (+)-salvianolic acid A. The current synthetic technology possesses the advantages of using inexpensive starting materials, mild reaction conditions and has the potential for use in large scale synthesis.
Synthesis of SMND-309, a derivate of salvianolic acid B
Wu, Kong,Song, Chan,Cui, Dong-Mei,Zhang, Chen
supporting information, p. 1387 - 1391 (2017/07/25)
(E)-2-(6-((E)-2-carboxyvinyl)-2,3-dihydroxyphenyl)-3-(3,4-dihydroxyphenyl) acrylic acid, designated SMND-309, was synthesized starting from 2-hydroxy-3-methoxybenzaldehyde in 12 steps and with an overall yield of 44%. The synthetic key features were the c
Method for synthesizing natural product salvianolic acid A methyl ester
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Paragraph 0079; 0080; 0081; 0082, (2017/07/20)
The invention relates to a novel method for synthesizing natural product salvianolic acid A methyl ester. A synthetic route is unique and novel in design; key strategies and steps comprise the step of using an easily-removed t-butyldimethylsilyl protectin
New synthesis method of natural product Salvianolic Acid F
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Paragraph 0014; 0031; 0032; 0033, (2018/01/04)
The invention discloses a new synthesis method of a natural product Salvianolic Acid F. The method comprises the following steps: carrying out hydroxyl group protection on 4-methycatechol used as a raw material, carrying out a methyl radical reaction, and
