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Showing posts with label SYNTHESIS. Show all posts
Showing posts with label SYNTHESIS. Show all posts

Friday, 29 July 2016

Ring-locking enables selective anhydrosugar synthesis from carbohydrate pyrolysis


Ring-locking enables selective anhydrosugar synthesis from carbohydrate pyrolysis

Green Chem., 2016, Advance Article
DOI: 10.1039/C6GC01600F, Paper
Li Chen, Jinmo Zhao, Sivaram Pradhan, Bruce E. Brinson, Gustavo E. Scuseria, Z. Conrad Zhang, Michael S. Wong
The nonselective nature of glucose pyrolysis chemistry can be controlled by preventing the sugar ring from opening and fragmenting.

Ring-locking enables selective anhydrosugar synthesis from carbohydrate pyrolysis

*Corresponding authors
aDepartment of Chemical and Biomolecular Engineering, Rice University, Houston, USA
E-mail: mswong@rice.edu
bDepartment of Chemistry, Rice University, Houston, USA
cDalian National Laboratory of Clean Energy, Dalian Institute of Chemical Physics, Dalian, China
E-mail: zczhang@dicp.ac.cn
dDepartment of Civil and Environmental Engineering, Rice University, Houston, USA
eDepartment of Materials Science and NanoEngineering, Rice University, Houston, USA
Green Chem., 2016, Advance Article
DOI: 10.1039/C6GC01600F
The selective production of platform chemicals from thermal conversion of biomass-derived carbohydrates is challenging. As precursors to natural products and drug molecules, anhydrosugars are difficult to synthesize from simple carbohydrates in large quantities without side products, due to various competing pathways during pyrolysis. Here we demonstrate that the nonselective chemistry of carbohydrate pyrolysis is substantially improved by alkoxy or phenoxy substitution at the anomeric carbon of glucose prior to thermal treatment. Through this ring-locking step, we found that the selectivity to 1,6-anhydro-β-D-glucopyranose (levoglucosan, LGA) increased from 2% to greater than 90% after fast pyrolysis of the resulting sugar at 600 °C. DFT analysis indicated that LGA formation becomes the dominant reaction pathway when the substituent group inhibits the pyranose ring from opening and fragmenting into non-anhydrosugar products. LGA forms selectively when the activation barrier for ring-opening is significantly increased over that for 1,6-elimination, with both barriers affected by the substituent type and anomeric position. These findings introduce the ring-locking concept to sugar pyrolysis chemistry and suggest a chemical-thermal treatment approach for upgrading simple and complex carbohydrates.
////////Ring-locking ,  selective anhydrosugar, carbohydrate pyrolysis, synthesis

Monday, 31 August 2015

Synthesis, physicochemical and biological evaluation of 2-amino-5-chlorobenzophenone derivatives as potent skeletal muscle relaxants


 

Rajesh Singh

M. Pharm., PhD, AIC
Professor (Assistant)

 

 link

 https://plus.google.com/115046907236504581005/about

 rksingh244@gmail.com

About

Dr Singh, educational qualifications from Panjab Univ., Chandigarh, GATE (2003) with 92.26 percentile, elected member of Association of Institution of Chemist (AIC), above 9 years of teaching experience and guided 16 PG students. He has to his credit > than 35 scientific research papers in reputed referred indexed journals, 40 res. presen., 1 book, 6 best paper presentation awards and 5 res. projects funded by PSCST, Chd. He is registered Pharmacist of Punjab State and life member of APTI.

Important pharmacophore of 1,4-benzodiazepine nucleus.
Figure 1.
Important pharmacophore of 1,4-benzodiazepine nucleus.




Synthesis of 2-amino-5-chloro-benzophenone derivatives (3a–3g)
Scheme 1.
Synthesis of 2-amino-5-chloro-benzophenone derivatives (3a3g)

2.3.3. 2-(4′-Chloroanilino)acetamido-5-chlorobenzophenone (3a)

IR (KBr cm−1): 3346 (Sec N–H str), 3100 (Aromatic C–H str), 2984 (Aliphatic C–H str), 1661 (Cdouble bond; length as m-dashO str), 1487 (Aromatic Cdouble bond; length as m-dashC str), 1229 (C–N str) and 761 (C–Cl str) 1H NMR (DMSO-d6 1δ ppm): 4.19 (s, 2H, –COCH2N), 7.26–8.60 (m, 12H, Ar–H) and 11.46 (br s, 1H, –NHCOCH2–) Anal. Calcd. for C21H16 N2O2Cl2: C, 63.17; H, 4.04; N, 7.02; Found: C, 63.07; H, 4.02; N, 7.09.

 1H NMR PREDICT





Volume 8, Issue 3, May 2015, Pages 307–312

Original article

Synthesis, physicochemical and biological evaluation of 2-amino-5-chlorobenzophenone derivatives as potent skeletal muscle relaxants

  • Pharmaceutical Chemistry Division, Shivalik College of Pharmacy, Nangal, Rupnagar, Punjab 140126, India
Open Access funded by King Saud University
Under a Creative Commons license
Rajesh Singh's profile photo
Corresponding author. Tel.: +91 01887 221276, mobile: +91 9417513730; fax: +91 01887 221276   rksingh244@gmail.com
1 Present Address: Dept. of Pharmaceutical Chemistry, Laureate Institute of Pharmacy, Kathog, Kangra, Himachal Pradesh, India.


Take a tour

 Pharmaceutical Chemistry Division, Shivalik College of Pharmacy, Nangal, Rupnagar, Punjab 140126, India












Dept. of Pharmaceutical Chemistry, Laureate Institute of Pharmacy, Kathog, Kangra, Himachal Pradesh, India.













 






Bhakra Dam, about 12 km from Nangal, the tallest dam of Asia


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Sunday, 16 March 2014

An efficient Cu(II)-bis(oxazoline)-based polymer immobilised ionic liquid phase catalyst for asymmetric carbon-carbon bond formation

An efficient Cu(II)-bis(oxazoline)-based polymer immobilised ionic liquid phase catalyst for asymmetric carbon-carbon bond formation

Green Chem., 2014, 16,1470-1479
DOI: 10.1039/C3GC41378K, Paper
Simon Doherty, Julian G. Knight, Jack R. Ellison, Peter Goodrich, Leanne Hall, Christopher Hardacre, Mark J. Muldoon, Soomin Park, Ana Ribeiro, Carlos Alberto Nieto de Castro, Maria Jose Lourenco, Paul Davey
Asymmetric carbon-carbon bond forming reactions were catalysed by heterogeneous copper(II)-bis(oxazoline)-based PIILP systems.


The asymmetric Diels–Alder reaction between N-acryloyloxazolidinone and cyclopentadiene and the Mukaiyama-aldol reaction between methylpyruvate and 1-phenyl-1-trimethylsilyloxyethene have been catalysed by heterogeneous copper(II)-bis(oxazoline)-based polymer immobilised ionic liquid phase (PIILP) systems generated from a range of linear and cross linked ionic polymers. In both reactions selectivity and ee were strongly influenced by the choice of polymer. A comparison of the performance of a range of Cu(II)-bis(oxazoline)-PIILP catalyst systems against analogous supported ionic liquid phase (SILP) heterogeneous catalysts as well as their homogeneous counterparts has been undertaken and their relative merits evaluated.

Wednesday, 16 October 2013

Microwave-assisted synthesis of N-heterocycles in medicinal chemistry


Med. Chem. Commun., 2013, 4,1323-1343
DOI: 10.1039/C3MD00152K, Review Article
Davide Garella, Emily Borretto, Antonella Di Stilo, Katia Martina, Giancarlo Cravotto, Pedro Cintas
Microwave-assisted synthesis of heterocycle libraries has given an impressive contribution to drug discovery and development.http://pubs.rsc.org/en/Content/ArticleLanding/2013/MD/C3MD00152K?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FMD+%28RSC+-+Med.+Chem.+Commun.+latest+articles%29#!divAbstract
 

Microwave-assisted synthesis of N-heterocycles in medicinal chemistry

 

 

 The syntheses of almost all N-heterocycles have now been successfully performed under microwave irradiation and have provided significant improvements in the reaction time and efficiency. The peculiar properties of dielectric heating give it the ability to strongly promote cyclocondensation, cycloaddition and selective N-heterocycle functionalisation and it has, therefore, very much caught the attention of the medicinal chemistry community. In this work, we present an overview of recent literature and technical advances in this research field with the aim of providing insight into the applications of microwave-assisted synthesis in the preparation of the main drug categories that contain N-heterocycle scaffolds.

Friday, 20 September 2013

Molecular Storage Provides Chlorine and Phosgene Safely

Molecular Storage Provides Chlorine and Phosgene Safely

Photodecomposition of tetrachloroethylene provides a safer source of small chlorinated building blocks for organic synthesis

Sunday, 1 September 2013

Synthesis of Tolvaptan

Synthesis of Tolvaptan


pick up all this at


YANG Chuanwei~1,MU Shuai~2,LIU Ying~3,WANG Pingbao~3,LIU Dengke~(3*) 
(1.School of Pharmacy,Henan University,Kaifeng 475004;2.
School of Chemical Engineering and Technology,
 Tianjin University,Tianjin 300072;3.
Tianjin Institute of Pharmaceutical Research,Tianjin 300193)  
Tolvaptan,a selective nonpeptide arginine vasopressin V_2 receptor antagonist,was synthesized
 from 7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine by acylation and reduction to give 1-(4-amino-2-methylbenzoyl) -7- chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine,which was subjected to acylation with 2-methylbenzoyl chloride and reduction with sodium borohydride with an overall yield of about 45%.
CAJViewer7.0 supports all the CNKI file formats; AdobeReader only supports the PDF format.
【Citations】
Chinese Journal Full-text Database2 Hits
1LI Fan1, HOU Xingpu2, LI Lin1, LU Tao1, DU Yumin1 (1. School of Pharmacy,
Hebei Medical University, Shijiazhuang 050017; 2. Shijiazhuang
 Pharma Group NBP Pharmaceutical Co., Ltd., Shijiazhuang 052160);
Synthesis of Antiparkinsonian Agent Istradefylline[J];Chinese Journal of Pharmaceuticals;2010-04
2YANG Miao~1,SHUAI Jun~2,LIU Mo~3,LIU Deng-ke~(3*),WANG Ping-bao~3
(1.Tianjin Medical University,Tianjin 300070;2.Tianjin University;Tianjin 300072;
 3.Tianjin Institute of Pharmaceutical Research,Tianjin 300193);
Synthesis of 7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine[J];
Chinese Journal of Pharmaceuticals;2009-09
【Co-citations】
Chinese Journal Full-text Database1 Hits
1XIONG Xiao-yi,CHEN An-qun,HE Yong-mei(Chongqing Unis Chemical Co.,Ltd.,Chongqing
402161,China);Analysis of Cyanoacetic Acid Content by HPLC[J];Guangzhou Chemical Industry;2010-12