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DR ANTHONY MELVIN CRASTO, WORLDDRUGTRACKER

A New Way to Treat Diabetes?

 diabetes, Uncategorized  Comments Off on A New Way to Treat Diabetes?
Jun 032014
 

thumbnail image: A New Way to Treat Diabetes?

http://www.chemistryviews.org/details/news/6210821/A_New_Way_to_Treat_Diabetes.html?utm_source=dlvr.it&utm_medium=facebook

Type-2 diabetes is a severe metabolic disease caused by the loss of the cells producing the hormone insulin. Since this molecule controls the up-take of glucose from the circulation, diabetic patients accumulate pathological levels of sugar in their blood.

 

 

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Amidation of phenol derivatives: a direct synthesis of paracetamol (acetaminophen) from hydroquinone

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May 302014
 

Green Chem., 2014, 16,2997-3002
DOI: 10.1039/C4GC00166D, Communication
Roxan Joncour, Nicolas Duguet, Estelle Metay, Amadeo Ferreira, Marc Lemaire
Paracetamol (acetaminophen) was prepared from hydroquinone and ammonium acetate in acetic acid with 88% yield and >99% purity.
A direct synthesis of paracetamol (acetaminophen) from hydroquinone has been developed using ammonium acetate as an amidating agent. The reaction proceeds in acetic acid at elevated temperatures without any metallic catalyst. Under these conditions, paracetamol was obtained with high yield and selectivity (>95%). The reaction has also been carried out on the multi-gram scale (44 g of hydroquinone) and a potential process has been proposed based on the recycling of the solvent and by-products. This amidation protocol has also been extended to other phenol derivatives.
ANTHONY MELVIN CRASTO

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Patient stem cells used to make ‘heart disease-on-a-chip’

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May 302014
 


Researchers use modified RNA transfection to correct genetic dysfunction in heart stem cells derived from Barth syndrome patients. The series of images show how inserting modified RNA into diseased cells causes the cells to produce functioning versions of the TAZ protein (first image: in green) that correctly localize in the mitochondria (second image: in red). When the images are merged to demonstrate this localization, green overlaps with red, giving the third image a yellow color. (Credit: Gang Wang and William Pu/Boston Children’s Hospital)

 

Harvard scientists have merged stem cell and ‘organ-on-a-chip’ technologies to grow, for the first time, functioning human heart tissue carrying an inherited cardiovascular disease. The research appears to be a big step forward for personalized medicine, as it is working proof that a chunk of tissue containing a patient’s specific genetic disorder can be replicated in the laboratory.

The work, published in Nature Medicine, is the result of a collaborative effort bringing together scientists from the Harvard Stem Cell Institute, the Wyss Institute for Biologically Inspired EngineeringBoston Children’s Hospital, the Harvard School of Engineering and Applied Sciences, and Harvard Medical School. It combines the ‘organs-on-chips’ expertise of Kevin Kit Parker, PhD, and stem cell and clinical insights by William Pu, MD.

read at

http://hsci.harvard.edu/news/patient-stem-cells-used-make-%E2%80%98heart-disease-chip%E2%80%99#.U4eNnBFG6qk.facebook

 

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1-((3-methoxyphenyl)sulfonyl)piperidine …learn spectroscopy

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May 152014
 

1-((3-methoxyphenyl)sulfonyl)piperidine (2) is a crystalline white solid

1-((3-Methoxyphenyl)sulfonyl)piperidine: Piperidine,

1-[(3-methoxyphenyl)sulfonyl]-; (2) cas no (173681-65-7)

mp 115-116 °C;

1H NMR pdf

(400 MHz, DMSO-d6, 2.50 ppm)

δ: 1.30-1.35 (m, 2 H, N(CH2CH2)2CH2),

1.47-1.52 (m, 4 H, N(CH2CH2)2CH2),

2.85 (t, J = 5.2 Hz, 4 H, N(CH2CH2)2CH2),

3.83 (s, 3 H, OMe),

7.16 (t, J = 2.1 Hz, 1 H, Ar-H),

7.25-7.30 (m, 2 H, Ar-H),

7.55 (t, J = 8.0 Hz, 1 H, Ar-H);

 

13C NMR pdf

(100 MHz, DMSO-d6, 39.5 ppm)

δ: 22.8, 24.7, 46.6, 55.6, 112.3, 118.7, 119.5, 130.5, 136.7, 159.5;

 

IR nmax (film)/cm-1 2940, 2851, 1597, 1478, 1359, 1340, 1318, 1287, 1241, 1167, 1098, 1040, 931, 856, 724, 688; (principal peaks);

HRMS (FTMS+p-NSF) found m/z 256.1002 [M+H]+, C12H18 NO3S requires m/z 256.1002.

 

Reverse phase HPLC analysis reveals purity >99% (run on an Agilent Zorbax SB-C18, 5 µm, 4.6 x 150 mm column (23 °C) at a flow rate of 1.5 mL/min of 75:25 MeCN:H2O observed at 210 nm giving a retention time of 1.95 min, 1.0 mg/mL in MeCN).

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NMR EXAMPLE

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May 152014
 

<br /><br />
			Reaction Scheme: <IMG src="/images/empty.gif">Deprotection of a tert-butyldimethylsilyl ether<IMG src="/images/empty.gif">

 

1H NMR (300 MHz; (CD3)2CO)
11.76 (1 H, s, OH (naph.) [exch]),
8.74 (1 H, dd, J 8.5 and 1.0, naph.),
8.10 (1 H, d, J 9.0, naph.),
7.89 (1 H, dd, J 8.5 and 1.5, naph.),
7.86 (1 H, dd, J 6.5 and 2.0, cyclop.),
7.59 (1 H, ddd, J 8.5, 7.0 and 1.5, naph.),
7.41 (1 H, ddd, J 8.5, 7.0 and 1.0, naph.),
7.22 (1 H, d, J 9.0, naph.),
6.50 (1 H, dd, J 6.5 and 2.0, cyclop.),
6.18 (1 H, q, J 2.0, cyclop.),
5.26 (1 H, d, J 5.5, OH (cyclop.) [exch]),
4.69 (1 H, dd, J 5.5 and 2.0, cyclop.)

 


Reference s

J. H. Clark, Chem. Rev., 1980, 80, 429 doi:10.1021/cr60327a004
E. J. Corey, A. Venkateswarlu, J. Am. Chem. Soc., 1972, 94, 6190 doi:10.1021/ja00772a043
A. B. Smith, III, G. R. Ott, J. Am. Chem. Soc., 1996, 118, 3095 (TBAF/AcOH)
K. C. Nicolaou, S. E. Webber, Synthesis, 1986, 453 (HF.py) doi:10.1055/s-1986-31673
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Biological Drug Works Against MERS Virus in Lab

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May 062014
 

 

This file photo provided by the National Institute for Allergy and Infectious Diseases shows a colorized transmission of the MERS coronavirus that emerged in 2012. Health officials on Friday, May 2, 2014 said the deadly virus from the Middle East has turned up for the first time in the U.S. (AP Photo/National Institute for Allergy and Infectious Diseases via The Canadian Press, File)

This file photo provided by the National Institute for Allergy and Infectious Diseases shows a colorized transmission of the MERS coronavirus that emerged in 2012. Health officials on Friday, May 2, 2014 said the deadly virus from the Middle East has turned up for the first time in the U.S. (AP Photo/National Institute for Allergy and Infectious Diseases via The Canadian Press, File)

read at

http://www.dddmag.com/news/2014/05/biological-drug-works-against-mers-virus-lab?et_cid=3921847&et_rid=523035093&type=cta

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