New Drug Approvals blog by Dr Anthony Crasto hits ten lakh views in 211 countries


New Drug Approvals hits ten lakh views in 211 countries



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Dr. Anthony Melvin Crasto
Principal Scientist, Glenmark Pharma


Highly selective hydrogenation and hydrogenolysis using a copper-doped porous metal oxide catalyst

Graphical abstract: Highly selective hydrogenation and hydrogenolysis using a copper-doped porous metal oxide catalyst

Highly selective hydrogenation and hydrogenolysis using a copper-doped porous metal oxide catalyst

A copper-doped porous metal oxide catalyst in combination with hydrogen shows selective and quantitative hydrogenolysis of benzyl ketones and aldehydes, and hydrogenation of alkenes.
A copper-doped porous metal oxide catalyst in combination with hydrogen shows selective and quantitative hydrogenolysis of benzyl ketones and aldehydes, and hydrogenation of alkenes. The approach provides an alternative to noble-metal catalysed reductions and stoichiometric Wolff-Kishner and Clemmensen methods.

Green Chem., 2015, Advance Article
DOI: 10.1039/C5GC01464F, Communication
Laurene Petitjean, Raphael Gagne, Evan S. Beach, Dequan Xiao, Paul T. Anastas!divAbstract

Highly selective hydrogenation and hydrogenolysis using a copper-doped porous metal oxide catalyst

*Corresponding authors
aYale University, Forestry & Environmental Studies, New Haven, USA
bUniversity of New Haven, New Haven, USA
Green Chem., 2015, Advance Article

DOI: 10.1039/C5GC01464F

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Paul T. Anastas

Director, Center for Green Chemistry and Green Engineering
Teresa and H. John Heinz III Professor in the Practice of Chemistry for the Environment, School of Forestry & Environmental Studies
Member of Yale faculty since 2007

Web site:

Research The objective of our research is to achieve increased understanding of the molecular basis of sustainability. Through an elucidation of the properties and interactions that lead to adverse consequence in the human body or in the biosphere, whether toxicological or physical, we can begin to address some of the concerns associated with chemicals in society. The design framework of the Principles of Green Chemistry seeks to optimize synthetic pathways and product design around minimum toxicity and material/energy inefficiency.

One of the specific focus areas of research interest is pursuing the generation of heuristic design rules for the construction of molecular structures of reduced hazard. By understanding the detailed mechanism of action of toxicity, it is possible to manipulate the properties regulating pharmacokinetics and pharmacodynamics in ways that reduce or eliminate the target biological endpoint. This framework is being applied to targets of high concern such as endocrine disruptors, persistent and bioaccumulating substances, and engineered nanostructures.

In process design of green chemistry systems, we seek to explore new chemical systems that accomplish efficient transformations and separations through the use of integrated synthetic and molecular engineering techniques.

B.S. University of Massachusetts, 1984
Ph.D. Brandeis University, 1989

Sustained Superior Performance Award, 1990
EPA Assistant Administrator’s Awards, 1991
Presidential Point of Light Award, 1991
Sustained Superior Performance Award, 1991
EPA Bronze Medal for Outstanding Service, 1993
Two EPA Bronze Medals for Outstanding Service, 1994
EPA Bronze Medal for Outstanding Service, 1995
First Annual Office of Pollution Prevention and Toxics Award for Outstanding Branch Chief, 1995
EPA Silver Medal – Design and Development EPA’s Green Chemistry Program, 1997
Vice-President’s Hammer Award – Green Chemistry Program, 1998
EPA Bronze Medal – Development of Green Chemistry Expert System, 1999
Nolan and Gloria Sommer Award – Distinguished Contributions to Chemistry, 1999
Joseph Seifter Award for Scientific Excellence in Risk Assessment, 1999
Vice President’s Hammer Award: Acute Exposure Guideline Levels Program, 2000
Honorary Professor, Queens University, Belfast, N. Ireland, 2001
Greek Chemical Society Award for Contributions to Chemistry, 2002
Erskine Scholar, University of Canterbury, New Zealand, 2002
Special Professor, Universitat of Vic, Barcelona, Spain, 2002
Inaugural Canadian Green Chemistry Medal, Montreal, Canada, 2004
“Scientific American 50” Award in Science and Technology, 2005
The Heinz Award, Environment, 2006
Bayer Distinguished Lectureship, 2007
Honorary Doctorate of Science in Chemistry, Queens University, Belfast, Ireland, 2007
John Jeyes Lectureship, UK Royal Society of Chemistry, 2007
Council of Scientific Society Presidents, 2008 Leadership in Science Award, 2008
Named to the “Nifty 50” Top Scientists by the U.S. Science and Engineering Festival, 2010
5th Annual Borlaug Lecturer, North Carolina State University, Raleigh, NC, 2010
Oppenheim Lecture, University of California at Los Angeles, 2011
Weber Distinguished Lecture in Energy and Environmental Sustainability, U. Michigan, 2011
Rachael Carson Award, Natural Products Association, 2011
Wöhler Prize, Gesellschaft Deutscher Chemiker (GDCh), 2012
Edward O. Wilson Biodiversity Technology Pioneer Prize, ACM, 2012

Recent Publications
K. Barta, G. Warner, E.S. Beach, & P.T. Anastas. Depolymerization of organosolv lignin to aromatic compounds over Cu-doped porous metal oxides. Green Chemistry 2014, 16 (1), 191-196.

A. Bloomfield, S. Sheehan, S. Collom, R. Crabtree, P.T. Anastas. A heterogeneous water oxidation catalyst from dicobalt octacarbonyl and 1,2-bis(diphenylphosphino)ethane. New Journal of Chemistry 2014, 38 (4), 1540-1545.

J. Kostal, A. Voutchkova-Kostal, P. Anastas, & J.B. Zimmerman. Identifying and designing chemicals with minimal acute aquatic toxicity. Proc Natl Acad Sci USA 2014.

G. Warner, T.S. Hansen, A. Riisager, E.S. Beach, K. Barta, & P.T. Anastas. Depolymerization of organosolv lignin using doped porous metal oxides in supercritical methanol. Bioresource Technology 2014, 161:78-83.

E.S. Beach, Z. Cui, P.T. Anastas, M. Zhan, & R.P. Wool. Properties of Thermosets Derived from Chemically Modified Triglycerides and Bio-Based Comonomers. Applied Sciences 2013, 3 (4), 684-693.

E.S. Beach, B.R. Weeks, R. Stern, & P.T. Anastas. Plastics additives and green chemistry. Pure and Applied Chemistry 2013, 85 (8), 1611-1624.

S.L. Collom, P.T. Anastas, E.S. Beach, R.H. Crabtree, N. Hazari, & T.J. Sommer. Differing Selectivities in Mechanochemical versus Conventional Solution Oxidation using Oxone. Tetrahedron Letters 2013, 54 (19), 2344-2347.

A. Kermanshahi pour, J. Zimmerman, & P. Anastas. Microalgae-derived chemicals: opportunity for an integrated chemical plant. In Natural and Artificial Photosynthesis: Solar Power as an Energy Source., Razeghifard, R. eds., Wiley, Inc, 2013.

A.M. Riederer, A. Belova, B.J. George, & P.T. Anastas. Urinary Cadmium in the 1999–2008 U.S. National Health and Nutrition Examination Survey (NHANES). Environmental Science & Technology 2013, 47 (2), 1137-1147.

I. Cote, P.T. Anastas, L.S. Birnbaum, R.M. Clark, D.J. Dix, S.W. Edwards, & P.W. Preuss. Advancing the Next Generation of Health Risk Assessment. Environmental Health Perspectives 2012, 120, 1499-1502.

T.S. Hansen, K. Barta, P.T. Anastas, P.C. Ford, & A. Riisager. One-pot reduction of 5-hydroxymethylfurfural via hydrogen transfer from supercritical methanol. Green Chemistry 2012, 14, 2457-2461.

A.M. Voutchkova-Kostal, J. Kostal, K.A. Connors, B.B. W, P.T. Anastas, & J.B. Zimmerman. Towards rational molecular design for reduced chronic aquatic toxicity. Green Chemistry 2012, 14, 1001-1008.

Z. Cui, E.S. Beach, & P.T. Anastas. Modification of chitosan films with environmentally benign reagents for increased water resistance. Green Chemistry Letters and Reviews 2011, 4, 35-40.

Z. Cui, E.S. Beach, & P.T. Anastas. Green chemistry in China. Pure and Applied Chemistry 2011, 83, 1379-1390.

P. Foley, A. Phimphachanh, E.S. Beach, J.B. Zimmerman, & P.T. Anastas. Linear and cyclic c-glycosides as surfactants. Green Chemistry 2011, 13, 321-325.

A.M. Voutchkova, J. Kostal, J.B. Steinfeld, J.W. Emerson, B.W. Brooks, P.T. Anastas, & J.B. Zimmerman. Towards rational molecular design: derivation of property guidelines for reduced acute aquatic toxicity. Green Chemistry 2011, 13, 2373-2379.

P. Foley, N. Eghbali, & P.T. Anastas. Advances in the methodology of a multicomponent synthesis of arylnaphthalene lactones. Green Chemistry 2010, 12, 888-892.

A.M. Voutchkova, L.A. Ferris, J.B. Zimmerman, & P.T. Anastas. Toward molecular design for hazard reduction-fundamental relationships between chemical properties and toxicity. Tetrahedron 2010, 66, 1031-1039.


Metal-free synthesis of polysubstituted oxazoles via a decarboxylative cyclization from primary α-amino acids


Scheme 1

Control experiments.

The ubiquitous oxazoles have attracted more and more attention in both industrial and academic fields for decades. This interest arises from the fact that a variety of natural and synthetic compounds which contain the oxazole substructure exhibit significant biological activities and antiviral properties. Although various synthetic methodologies for synthesis of oxazols have been reported, the development of milder and more general procedure to access oxazoles is still desirable.

Initially, compound A, formed by the substitution reaction of 1a with 2a, which can be transformed following two pathways: (a) I+, generated by the oxidation of iodine, could oxidize A to radical intermediate B, which eliminates one molecular of CO2 to generate radical C, which is further oxidized to imine Dor its isomer E. Subsequently, F is obtained by intramolecular nucleophilic addition of E. Finally, the desired product…

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lei gong teng ,:雷公藤, Tripterygium wilfordii Hook F. for Rheumatoid Arthritis

New Drug Approvals

A Chinese herb called thunder god vine works better than a widely-prescribed pharmaceutical drug at easing rheumatoid arthritis, a new study has found.

Tripterygium regelii, Aizu area, Fukushima pref, Japan

The herb has long been used in China to treat this potentially crippling autoimmune disease, which typically strikes hand and foot joints. It is known in Mandarin as ‘lei gong teng’ and to botanists as Tripterygium wilfordii Hook F.

Extracts of the herb have already fired the interest of drug laboratories as they contain hundreds of compounds, including intriguing molecules called diterpenoids which are believed to ease inflammation and immune response.

read at


Researchers at the Johns Hopkins School of Medicine have discovered that a natural constituent isolated from a traditional Chinese medicinal herb, Triptergium wilfordii Hook F. (雷公藤, Lei Gong Teng, Thunder God Vine), used for hundreds of years to treat many conditions, works well by blocking gene control machinery in the…

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Eco-friendly synthesis of diverse and valuable 2-pyridones by catalyst- and solvent-free thermal multicomponent domino reaction


An efficient and highly eco-friendly synthesis of diverse and functionalized 2-pyridone derivatives in good yield via the thermal multicomponent reaction of 4-oxo-4H-chromene-3-carbaldehydes with 1,3-diketoesters and anilines or primary aliphatic amines under catalyst- and solvent-free conditions is described. This reaction proceeds via domino Knoevenagel condensation/Michael addition/ring opening/ring closure reactions.

Eco-friendly synthesis of diverse and valuable 2-pyridones by catalyst- and solvent-free thermal multicomponent domino reaction

Green Chem., 2015, 17,4579-4586
DOI: 10.1039/C5GC01526J, Paper
Tej Narayan Poudel, Yong Rok Lee, Sung Hong Kim!divAbstract
An eco-friendly protocol for diverse and functionalized 2-pyridone derivatives via a multicomponent reaction under catalyst- and solvent-free conditions has been developed.

nmr, structures



How flow chemistry can make processes greener.. Case study 1 Methylation with DMC.

Figure . Flow chart carboxylate system (B = vessel, V = valve).

Alkylation of N methylimidazole (MIM) with dimethyl carbonate (DMC) is investigated. Dimethyl carbonate is known as a clean methylation agent which can be used as safe alternative to conventional reagents such as methyl halides, dimethyl sulfate and phosgene. With the system shown in Figure 4, which is operated continuously, it is possible to synthesize the zwitterion 1,3-dimethyl-1H-imidazol-3-ium-2-carboxylate ([MMIM][CO2]) by alkylation of MIM with DMC. Similarly, the synthesis of ionic liquids based on N methylpiperidine and N methylpyrrolidine is possible. These ionic liquids represent versatile precursors for the synthesis of halogen free ionic liquids.

How flow chemistry can make processes greener

Case study 1 Methylation with DMC.

Increasing reaction efficiency through access to a wider range of reaction conditions

Efficient utilization of energy and time is fundamental to green chemistry and engineering. These factors are directly related to the rate of a chemical reaction, as a fast reaction will require less operating time. Economical use of space is also important, and fast reactions may allow for a smaller reactor to be utilized, particularly in continuous processes. The most straightforward way to increase reaction rate is with an increase in temperature; however, in a batch reactor, this is generally limited to the atmospheric boiling point of the solvent or reagents. In a flow reactor, pressure and temperature can be safely manipulated far beyond atmospheric conditions. Analogous to microwaves synthesis,1 reactions done in flow are often faster than in the corresponding batch reactions, which gives improved energy, time, and space efficiency.1 In contrast to typical microwave reactors, a closed system is not required, greatly facilitating scale-up.

Methylation reactions of nitrogen and oxygen nucleophiles such as indoles and phenols are important transformations often carried out on a large scale using hazardous reagents such as methyl iodideor dimethyl sulfate . Dimethylcarbonate (DMC) has been recognized as a green, albeit less reactive alternative. Due to the relatively low boiling point (90 °C) and reduced reactivity of this reagent, methylation reactions with DMC are generally slow.3 The use of an autoclave or microwave may allow higher temperatures to be used, accessing faster rates; however, this makes scale-up challenging. To access fast reaction rates and improve scalability, Tilstam used a flow reactor to do phenol and N-heterocycle methylations with DMC.4 A simple set-up was used consisting of a high pressure syringe pump, stainless steel tubing, a GC oven, and a back pressure regulator to ensure that the DMC stayed in solution. At 220 °C, yields up to 97% could be obtained with reaction times as short as ten minutes. A report by the Kappe and Holbrey group found similar results using an ionic liquid catalyst.5 While more energy may be required to reach these elevated temperatures, the use of insulation to prevent heat loss, and recycling of the energy given off from exothermic reactions all contribute greatly to energy efficiency on a commercial scale.6 Perhaps most importantly, the reduction in size and operating time of the vessel offers great improvements in sustainability. Indeed, the output of a reactor with respect to its size and operating time was identified as the most impactful component of a good process by researchers at Boehringer Ingelheim.7


Methylation with DMC.
Scheme 1 Methylation with DMC.
  1. Microwaves in Organic Synthesis, ed. A. Loupy, Wiley-VCH, Weinheim, 2006 Search PubMed.
  2. T. Razzaq and C. O. Kappe, Chem.–Asian. J., 2010, 5, 1274–1289 CAS.
  3. W.-C. Shieh, S. Dell and O. Repič, Org. Lett., 2001, 3, 4279–4281 CrossRef CAS.
  4. U. Tilstam, Org. Process Res. Dev., 2012, 16, 1974–1978 Search PubMed.
  5. T. N. Glasnov, J. D. Holbrey, C. O. Kappe, K. R. Seddon and T. Yan, Green Chem., 2012, 14, 3071–3076 RSC.
  6. S. Heubschmann, D. Kralisch, V. Hessel, U. Krtschil and C. Kompter, Chem. Eng. Technol., 2009, 32, 1757–1765 CrossRef CAS.
  7. R. Dach, J. J. Song, F. Roschanger, W. Samstag and C. H. Senanayake, Org. Process Res. Dev., 2012, 16, 1697–1706 Search PubMed.


Carbon dioxide (CO2) is an easily available, renewable carbon resource, which has the advantages of being non-toxic, abundant and economical. CO2 is also attractive as an environmentally friendly chemical reagent, and is especially useful as a phosgene substitute.CO2 is an “anhydrous carbonic acid” that rapidly reacts with basic compounds. Nucleophilicattack at CO2 conveniently produces carboxyl and carbamoyl groups. Further reactions of these species with electrophiles lead to the formation of organic carbonates and carbamates. The present article deals with the synthetic technologies leading to organic carbonates using CO2 as a raw material.


Graphical abstract: The synthesis of organic carbonates from carbon dioxide

The synthesis of organic carbonates from carbon dioxide

*Corresponding authors
aNational Institute of Advanced Industrial Science and Technology (AIST), AIST Central 5, 1-1-1 Higashi, Japan
Fax: +81 29-861-4719
bGraduate School of Pure and Applied Sciences, University of Tsukuba, Tennodai 1-1-1, Tsukuba, Ibaraki 305-8571, Japan
Chem. Commun., 2009, 1312-1330

DOI: 10.1039/B819997C

Solvent-free Mizoroki–Heck reactions and its application in the synthesis of Axitinib

A green method for the synthesis of a D-glucosamine-derived triazole@palladium catalyst is described. The synthesized catalyst containing a 2-pyridyl-1,2,3-triazole ligand was prepared via a click route in high yields and was explored in Heck cross-coupling reactions between different aryl halides and olefins under solvent-free conditions. The catalyst can be separated from the reaction mixture and reused at least six times with superior activity. In addition, using this protocol, the marketed drug Axitinib (antitumor) could be synthesized easily.


Graphical abstract: A novel d-glucosamine-derived pyridyl-triazole@palladium catalyst for solvent-free Mizoroki–Heck reactions and its application in the synthesis of Axitinib

A novel D-glucosamine-derived pyridyl-triazole@palladium catalyst for solvent-free Mizoroki–Heck reactions and its application in the synthesis of Axitinib

Chao Shen,ab   Hongyun Shen,b   Ming Yang,b   Chengcai Xiab and   Pengfei Zhang*b  

*Corresponding authors
aCollege of Biology and Environmental Engineering, Zhejiang Shuren University, Hangzhou 310015, China
bCollege of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou 310036, China
Fax: +86-571-28862867
Tel: +86-571-28862867
Green Chem., 2015,17, 225-230

DOI: 10.1039/C4GC01606H