Welcome Scientific update to Pune, India 2-3 and 4-5 Dec 2014 for celebrating Process chemistry

New Drug Approvals

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TRAINING COURSE   2-3 DEC 2014

Process Development for Low Cost Manufacturing

When:02.12.2014 – 03.12.2014

Tutors:

• Dr John Knight, Scientific Update
• Dr Will Watson, Scientific Update 

Where: National Chemical Laboratory – Pune, India

Brochure:View Brochure

Register http://scientificupdate.co.uk/training/scheduled-training-courses.html

DESCRIPTION

Chemical process research and development is recognised as a key function during the commercialisation of a new product particularly in the generic and contract manufacturing arms of the chemical, agrochemical and pharmaceutical industries.

The synthesis and individual processes must be economic, safe and must generate product that meets the necessary quality requirements.

This 2-day course presented by highly experienced process chemists will concentrate on the development and optimisation of efficient…

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Mesoporous carbon nitride grafted with n-bromobutane: a high-performance heterogeneous catalyst for the solvent-free cycloaddition of CO2 to propylene carbonate

Catal. Sci. Technol., 2014, Advance Article
DOI: 10.1039/C4CY00770K, Paper

Jie Xu, Fei Wu, Quan Jiang, Yong-Xin Li
Mesoporous carbon nitride grafted n-bromobutane shows high catalytic activity in the solvent-free cycloaddition of CO₂ with propylene oxide to propylene carbonate, affording a maximum yield of 88% with a TOF up to 10.7 h^-1.

http://pubs.rsc.org/en/Content/ArticleLanding/2014/CY/C4CY00770K?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2Fcy+%28RSC+-+Catalysis+Science+%26+Technology+latest+articles%29#!divAbstract

Mesoporous carbon nitride grafted with n-bromobutane: a high-performance heterogeneous catalyst for the solvent-free cycloaddition of CO2 to propylene carbonate

Jie Xu,*a Fei Wu,a Quan Jianga and Yong-Xin Li*a

*Corresponding authors
aJiangsu Key Laboratory of Advanced Catalytic Materials and Technology, College of Chemistry and Chemical Engineering, Changzhou University, Gehu Road 1, Changzhou, PR China
E-mail: shine6832@163.com, liyxluck@163.com;
Fax: +86 519 86330135 ;
Tel: +86 519 86330135
Catal. Sci. Technol., 2014, Advance Article
DOI: 10.1039/C4CY00770K

A new type of mesoporous-C4N4-based catalyst (n-butBr/mp-C3N4) was prepared by simple grafting of n-bromobutane. The N2 adsorption–desorption and X-ray diffraction characterizations indicate that, in comparison with the parent mp-C3N4, the textual and structural properties have been well retained by n-butBr/mp-C3N4. In the cycloaddition of CO2 with propylene epoxide, the n-butBr/mp-C3N4 exhibits high catalytic conversion as well as a high selectivity to propylene carbonate. The maximum TOF value obtained over n-butBr/mp-C3N4 is 10.7 h−1 at 6 h under 140 °C, which compares favorably to other reported C3N4-based catalysts. In addition to n-bromobutane, mp-C3N4 materials grafted with other alkyl halides also provide high catalytic activities. According to the Fourier transform infrared and X-ray photoelectron spectroscopy measurements, it is speculated that the catalytic active sites of n-butBr/mp-C3N4 are uncondensed amines and Br anions which originate from the reaction between n-bromobutane and the N-containing heterocycles of mp-C3N4.

  MAKE IN INDIA
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Efficient synthesis of supported proline catalysts for asymmetric aldol reactions

Proline has been grafted onto silica supports in a single step by reacting trans-4-hydroxy-L-proline with chloropropyl tethers, without the use of protecting groups for the proline amine and carboxylic acid functional groups. The resulting catalysts have been characterised to show that grafting is through reaction with the 4-hydroxy group. The catalysts have been tested in an asymmetric aldol reaction, and shown to be both more active and more enantioselective than equivalent catalysts prepared using a protection/deprotection route for the proline grafting step.

http://pubs.rsc.org/en/Content/ArticleLanding/2014/CY/C4CY00970C?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2Fcy+%28RSC+-+Catalysis+Science+%26+Technology+latest+articles%29#!divAbstract

Efficient synthesis of supported proline catalysts for asymmetric aldol reactions
A. A. Elmekawy,a J. B. Sweeneya and D. R. Brown*a

*Corresponding authors
aDepartment of Chemical Sciences, University of Huddersfield, Huddersfield HD1 3DH, UK
E-mail: d.r.brown@hud.ac.uk;
Fax: +44 (0)1484 472182 ;
Tel: +44 (0)1484 47339
Catal. Sci. Technol., 2014, Advance Article
DOI: 10.1039/C4CY00970C

INCB-039110, Janus kinase-1 (JAK-1) inhibitor……..for the treatment of rheumatoid arthritis, myelofibrosis, rheumatoid arthritis and plaque psoriasis.

New Drug Approvals

INCB-39110,

CAS 1334298-90-6

INCB-039110, Jak1 tyrosine kinase inhibitor

3-​Azetidineacetonitril​e, 1-​[1-​[[3-​fluoro-​2-​(trifluoromethyl)​-​4-​pyridinyl]​carbonyl]​-​4-​piperidinyl]​-​3-​[4-​(7H-​pyrrolo[2,​3-​d]​pyrimidin-​4-​yl)​-​1H-​pyrazol-​1-​yl]​-

 C₂₆H₂₃F₄N₉O (MW, 553.51)

{ l- { l-[3-fluoro-2- (trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4- yl)-lH-pyrazol-l-yl]azetidin-3-yl}acetonitrile

2-(3-(4-(7H-pyrrolo[2,3-( Jpyrimidin-4-yl)-lH- pyrazol- 1 -yl)- 1 -( 1 -(3 -fluoro-2-(trifluoromethyl)isonicotinoyl)piperidin-4-yl)azetidin- 3-yl)acetonitrile

2-(3-(4-(7H- Pyrrolo[2,3 -i/]pyrimidin-4-yl)- lH-pyrazol- 1 -yl)- 1 -(1 -(3 -fluoro-2- (trifluoromethyl)isonicotinoyl)piperidin-4-yl)azetidin-3-yl)acetonitrile adipate MAY BE THE DRUG… HAS CAS 1334302-63-4

ADIPATE OF INCB-39110

ALSO/OR

3-​Azetidineacetonitril​e, 1-​[1-​(3-​fluorobenzoyl)​-​4-​methyl-​4-​piperidinyl]​-​3-​[4-​(7H-​pyrrolo[2,​3-​d]​pyrimidin-​4-​yl)​-​1H-​pyrazol-​1-​yl]​-​, 2,​2,​2-​trifluoroacetateMAY BE THE DRUG ????…  HAS CAS  1334300-52-5

US 2011/0224190

Incyte Corporation

IN PHASE 2 for the treatment of rheumatoid arthritis, myelofibrosis, rheumatoid arthritis and plaque psoriasis.

SEE

http://clinicaltrials.gov/show/NCT01633372

Jak2 tyrosine kinase inhibitor; Jak1 tyrosine kinase inhibitor

Breast tumor; Chronic obstructive pulmonary disease; Crohns disease; Inflammatory bowel disease; Influenza virus infection; Insulin dependent diabetes; Liver tumor; Multiple sclerosis; Prostate tumor; Rheumatoid arthritis; SARS coronavirus infection

Used for treating cancers (eg prostate cancer, hepatic cancer…

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Mild and selective heterogeneous catalytic hydration of nitriles to amides by flowing through manganese dioxide

Mild and selective heterogeneous catalytic hydration of nitriles to amides by flowing through manganese dioxide

C. Battilocchio, J.M. Hawkins, S.V. Ley, Org. Lett. 2014, 16, 1060-1063.

Claudio Battilocchio †, Joel M. Hawkins ‡, andSteven V. Ley *†

^† Innovative Technology Centre, Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW, Cambridge U.K.

^‡ Pfizer Worldwide Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States

Org. Lett., 2014, 16 (4), pp 1060–1063

DOI: 10.1021/ol403591c

http://pubs.acs.org/doi/abs/10.1021/ol403591c

A sustainable flow chemistry process for the hydration of nitriles, whereby an aqueous solution of the nitrile is passed through a column containing commercially available amorphous manganese dioxide, has been developed. The product is obtained simply by concentration of the output stream without any other workup steps. The protocol described is rapid, robust, reliable, and scalable, and it has been applied to a broad range of substrates, showing a high level of chemical tolerance.

Red wine compound could help seniors walk away from mobility problems

CLINICALNEWS.ORG

PHILADELPHIA, Aug. 19, 2012 — In a stride toward better health in later life, scientists reported today that resveratrol, the so-called “miracle molecule” found in red wine, might help improve mobility and prevent life-threatening falls among older people. The finding, believed to be the first of its kind, was presented today to some 14,000 scientists and others gathered at the 244thNational Meeting & Exposition of the American Chemical Society, the world’s largest scientific society.

The researchers say this report — based on studies of laboratory mice — could lead to the development of natural products designed to help older Americans live safer and more productive lives.

“Our study suggests that a natural compound like resveratrol, which can be obtained either through dietary supplementation or diet itself, could actually decrease some of the motor deficiencies that are seen in our aging population,” said Jane E. Cavanaugh, Ph.D., leader of the research…

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.Continuous preparation of arylmagnesium reagents in flow with in-line IR monitoring

.Continuous preparation of arylmagnesium reagents in flow with in-line IR monitoring

T. Brodmann, P. Koos, A. Metzger, P. Knochel, S.V. Ley, Org. Proc. Res. Dev. 2012, 16, 1102-1113.

http://pubs.acs.org/doi/abs/10.1021/op200275d

A newly developed microscale ReactIR flow cell was used as a convenient and versatile inline analytical tool for Grignard formation in continuous flow chemical processing. The LiCl-mediated halogen/Mg exchange reaction was used for the preparation of functionalized arylmagnesium compounds from aryl iodides or bromides. Furthermore, inline IR monitoring was used for the analysis of conversion and possible byproduct formation, as well as a potential tool for elucidation of mechanistic details. The results described herein indicate that the continuous flow systems are effective for highly exothermic reactions such as the Grignard exchange reaction due to fast mixing and efficient heat transfer.

Copying Nature’s Assembly Line Organic Synthesis: Successive homologation reactions let chemists tailor carbon chain’s conformation

Reaction repeatedly inserts organolithium compound into carbon-boron bond, creating chains up to 10 carbons long.

http://cen.acs.org/articles/92/i37/Copying-Natures-Assembly-Line.html
Reaction repeatedly inserts organolithium compound into carbon-boron bond, creating chains up to 10 carbons long

Copying Nature’s Assembly Line

Organic Synthesis: Successive homologation reactions let chemists tailor carbon chain’s conformation
Organic chemists have long admired nature for its ability to perform chemistry in an assembly-line style, wherein the same reaction or sets of reactions are carried out repeatedly to create a target molecule. Polyketide natural products, for example, are biosynthesized via such an assembly-line process.
Now, chemists at England’s University of Bristol report an assembly-line reaction that can be done in a flask (Nature 2014, DOI: 10.1038/nature13711).

 

Studies of a diastereoselective electrophilic fluorination reaction employing a cryo-flow reactor

Studies of a diastereoselective electrophilic fluorination reaction employing a cryo-flow reactor

K. Nakayama, D.L. Browne, I.R. Baxendale, S.V. Ley, Synlett 2013, 24, 1298-1302.

https://www.thieme-connect.de/DOI/DOI?10.1055/s-0033-1338455

The application of meso-scale flow chemistry in research laboratories continues to increase. Here, we report on the use of a modular cryo-flow device as applied to a diastereoselective fluorination process. The reactor can be incorporated into existing flow chemistry setups to permit continuous processing at low temperatures without recourse to cryogenic consumables.

Azaheterocycles Made Easy

Azaheterocycles Made Easy
Flexible route makes azaheterocycles easier to access

 

Azaheterocycles are a highly important class of compounds due to their biological activities and pharmaceutical applications. In particular, dihydroazepines, dihydropyrroles, and pyrroles are constituents of a valuable privileged structure in organic chemistry.

Read more

 

http://www.chemistryviews.org/details/ezine/6508611/Azaheterocycles_Made_Easy.html