Jiadifenolide synthesis

Naturalproductman's Blog

Erik Sorensen and co-workers reported in ACIE on the synthesis of jiadifenolide.
jiadifenolideACIE paper

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Enzyme that silences DNA activity may be crucially involved in health and cancer

Lyra Nara Blog

Genomics: The significance of silence

Understanding the action of Wip1, an enzyme that controls DNA silencing, could help explain both the development of cancer and resistance to anticancer drugs. Credit: Svisio/iStock/Thinkstock

Cancers can develop when the complex molecular networks that control the activity of DNA are disrupted. Researchers from the A*STAR Institute of Molecular and Cell Biology in Singapore, led by Dmitry Bulavin, have studied Wip1, an enzyme central to these molecular networks that may both help to keep cells healthy but also become part of the problem when things go wrong. The team’s findings suggest that this enzyme, and its associated signaling pathways, could be a target for the development of new drugs to combat some types of cancer. They may also explain why some cancers are resistant to drug therapy.

Bulavin and co-workers uncovered the role of the Wip1 enzyme when examining the deactivation or ‘silencing’ of regions of DNA by DNA methylation…

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ACT-280778 is a L/T calcium channel blocker potentially indicated for the treatment of hypertension and angina pectoris

New Drug Approvals

Abstract Image

ACT-280778

(1R,2R,4R)-2-(2-((3-(4,7-Dimethoxy-1H-benzo[d]imidazol-2-yl)propyl)(methyl)amino)ethyl)-5-phenylbicyclo[2.2.2]oct-5-en-2-yl Isobutyrate

Propanoic acid, 2-​methyl-​, (1R,​2R,​4R)​-​2-​[2-​[[3-​(4,​7-​dimethoxy-​1H-​benzimidazol-​2-​yl)​propyl]​methylamino]​ethyl]​-​5-​phenylbicyclo[2.2.2]​oct-​5-​en-​2-​yl ester

isobutyric acid (1R,2R,4R)-2-(2-{[3-(4,7-dimethoxy-1H-benzoimidazol-2-yl)-propyl]-methyl-amino}-ethyl)-5-phenyl-bicyclo[2.2.2]oct-5-en-2-yl ester

Actelion Pharmaceuticals Ltd innovator

C33 H43 N3 O4 1075744-31-8

bis-MALEATE SALT  1537197-53-7

Chiral bicyclic benzimidazole 1 (ACT-280778) is a L/T calcium channel blocker potentially indicated for the treatment of hypertension and angina pectoris 

 Many cardiovascular disorders have been associated with a ‘calcium overload’ resulting from an abnormal elevated calcium influx through the plasma membrane of cardiac and vascular smooth muscle cells. There are 3 major pathways through which extracellular calcium can enter these cells: 1 ) receptor-activated calcium channels, 2) ligand-gated calcium channels and 3) voltage-operated calcium channels (VOCs). 0 VOCs have been classified into 6 main categories: L (Long-lasting), T (Transient), N (Neuronal), P (Purkinje cells), Q (after P) and R…

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Inexpensive ionic liquids: [HSO4]−-based solvent production at bulk scale

Inexpensive ionic liquids: [HSO4]–based solvent production at bulk scale

Green Chem., 2014, Advance Article
DOI: 10.1039/C4GC00016A, Paper
Long Chen, Mahdi Sharifzadeh, Niall Mac Dowell, Tom Welton, Nilay Shah, Jason P. Hallett
ILs manufactured from inexpensive raw materials in few steps are cheaper than some organic solvents and have a low environmental impact.
Green Chem., 2014, Advance Article

DOI: 10.1039/C4GC00016A

Through more than two decades’ intensive research, ionic liquids (ILs) have exhibited significant potential in various areas of research at laboratory scales. This suggests that ILs-based industrial process development will attract increasing attention in the future. However, there is one core issue that stands in the way of commercialisation: the high cost of most laboratory-synthesized ILs will limit application to small-scale, specialized processes. In this work, we evaluate the economic feasibility of two ILs synthesized via acid–base neutralization using two scenarios for each: conventional and intensification processing. Based upon our initial models, we determined the cost price of each IL and compared the energy requirements of each process option. The cost prices of triethylammonium hydrogen sulfate and 1-methylimidazolium hydrogen sulfate are estimated as $1.24 kg−1 and $2.96–5.88 kg−1, respectively. This compares favourably with organic solvents such as acetone or ethyl acetate, which sell for $1.30–$1.40 kg−1. Moreover, the raw materials contribute the overwhelming majority of this cost and the intensified process using a compact plate reactor is more economical due to lower energy requirements. These results indicate that ionic liquids are not necessarily expensive, and therefore large-scale IL-based processes can become a commercial reality.

Cyanoformate Structure Could Aid Efforts To Trap Carbon Dioxide

Ball-and-stick structure of tetraphenylphosphonium cyanoformate.

Tetraphenylphosphonium (left) enabled the capture of the elusive cyanoformate anion (right).

Cyanoformate Structure Could Aid Efforts To Trap Carbon Dioxide

Unstable Complex: Elusive ion’s unusual bonding could inform design of agents that capture greenhouse gas.

read at

http://cen.acs.org/articles/92/i14/Cyanoformate-Structure-Aid-Efforts-Trap.html

Salt Additives Can Be Used To Tailor Negishi Cross-Couplings

Reaction scheme shows how a salt additive such as LiCl is necessary in some cases for Negishi cross-couplings to succeed.

SALT TO TASTE
A salt additive such as LiCl is necessary in some cases for Negishi cross-couplings to succeed.

Salt Additives Can Be Used To Tailor Negishi Cross-Couplings

Organic Synthesis: Chemists find that adding a salt affects aryl- and alkylzinc reagents differently.

 

read at

http://cen.acs.org/articles/92/i14/Salt-Additives-Used-Tailor-Negishi.html

 

13C NMR OF SIMPLE MOLECULES…………..Brush up….???

New Drug Approvals

ما هو هذا، لماذا أنت قلق، فرشاة مع الأشياء البسيطة، وسوف يخرج عبقري، وتعلم معي، قطرات صغيرة من الماء جعلالمحيطات، وسوف يكون خبيرا في هذا

what is this, why are you worried, brush up with simple things, you will come out genius, learn with me, small drops of water make an ocean, you will be an expert in this

あなたが心配している理由は、これは簡単なことでブラッシュアップ、、何か、あなたは、天才が出てくる私と一緒に学ぶことが、水の小さな滴が海を作るには、この専門家になる

structure

Name: 1,2-dimethoxymethane

C4H10O2

From the molecular formula, the compound has “0 degrees of unsaturation” (no double bonds or rings).

C13 SpectrumThe 13C NMR has two peaks, a quartet at  54 (a CH3) and a triplet at  80 (a CH2). Since the molecule has four carbons and only two 13C NMR peaks, there must be symmetry. Both peaks are in the regions where carbons next to electronegative atoms occur…

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