DR ANTHONY MELVIN CRASTO,WorldDrugTracker, helping millions, A 90 % paralysed man in action for you, I am suffering from transverse mylitis and bound to a wheel chair, With death on the horizon, nothing will not stop me except God
DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 30 Yrs Exp. in the feld of Organic Chemistry. Serving chemists around the world. Helping them with websites on Chemistry.Millions of hits on google, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution

Monday, 26 January 2015

Synthesis of Prostaglandin Analogues, Latanoprost and Bimatoprost, Using Organocatalysis via a Key Bicyclic Enal Intermediate


Synthesis of Prostaglandin Analogues, Latanoprost and Bimatoprost, Using Organocatalysis via a Key Bicyclic Enal Intermediate

School of Chemistry, University of Bristol, Cantock’s Close, Bristol, BS8 1TS, U.K.
Org. Lett., Article ASAP
DOI: 10.1021/ol503520f
Publication Date (Web): January 12, 2015
Copyright © 2015 American Chemical Society

Two antiglaucoma drugs, bimatoprost and latanoprost, which are analogues of the prostaglandin, PGF, have been synthesized in just 7 and 8 steps, respectively. The syntheses employ an organocatalytic aldol reaction that converts succinaldehyde into a key bicyclic enal intermediate, which is primed for attachment of the required lower and upper side chains. By utilizing the crystalline lactone, the drug molecules were prepared in >99% ee.

Image result for univ of bristol
Professor Varinder Aggarwal

Professor Varinder Aggarwal 
BA, PhD(Cantab), FRS


Area of research

Asymmetric synthesis, methodology and applications.

Asymmetric synthesis, methodology and applications.

My research interests include; the development of new catalytic processes for asymmetric synthesis; the development of chiral carbenoids and their use and subsequent applications in catalysis and synthesis; the development of new methodology and its applications in synthesis; total synthesis of biologically important targets.

Research keywords

  • catalytic processes
  • asymmetric synthesis
  • reactive intermediates
  • synthesis
  • carbenes
  • carbenoids

Latest publications

Map of University of Bristol, Cantock's Cl, Bristol, City of Bristol BS8 1TS, UK

Cantock's Close


Monday, 12 January 2015

Efficient Metathesis of Terminal Alkynes


Efficient Metathesis of Terminal Alkynes (pages 13019–13022)
Dipl.-Chem. Birte Haberlag, Dr. Matthias Freytag, Dr. Constantin G. Daniliuc, Prof. Dr. Peter G. Jones and Prof. Dr. Matthias Tamm
Article first published online: 14 NOV 2012 | DOI: 10.1002/anie.201207772
Thumbnail image of graphical abstract
Now even terminal: The 2,4,6-trimethylbenzylidyne complexes [MesC[TRIPLE BOND]M{OC(CF3)2Me}3] (M=Mo, W) were synthesized from [Mo(CO)6] and [W(CO)6], respectively. The molybdenum complex is an efficient catalyst for the metathesis of internal and terminal alkynes and also for the ring-closing metathesis of internal and terminal α,ω-diynes at room temperature and low catalyst concentrations.

Sunday, 11 January 2015

"Cyclizative Atmospheric CO2 Fixation by Unsaturated Amines with t-BuOI Leading to Cyclic Carbamates"

"Cyclizative Atmospheric CO2 Fixation by Unsaturated Amines with t-BuOI Leading to Cyclic Carbamates"
Youhei Takeda, Sota Okumura, Saori Tone, Itsuro Sasaki, and Satoshi Minakata*
Org. Lett. 201214, 4874–4877. DOI: 10.1021/ol302201q 

* Highlighted in "Noteworthy Chemistry" (ACS, October 1, 2012)! see the detail
Abstract: A cyclizative atmospheric CO2 fixation by unsaturated amines such as allyl and propargyl amines under mild reaction conditions, efficiently leading to cyclic carbamates bearing a iodomethyl group, have been developed utilizing tert-butyl hypoiodite (t-BuOI).

Thursday, 8 January 2015

Continuous Synthesis of Organozinc Halides Coupled to Negishi Reactions

Continuous Synthesis of Organozinc Halides Coupled to Negishi


 Article first published online: 20 JUN 2014

DOI: 10.1002/adsc.201400243


Advanced Synthesis & Catalysis

Volume 356Issue 18pages 3737–3741December 15, 2014

Nerea Alonso2,3,

L. Zane Miller1,

Juan de M. Muñoz2,

Jesus Alcázar2,*

D. Tyler McQuade1,*

1Department of Chemistry and Biochemistry, Florida State University, USA
2Janssen Research and Development, Janssen-Cilag, Toledo, Spain
3Facultad de Química, Universidad de Castilla-La Mancha, Spain

The Negishi cross-coupling is a powerful CC bond forming reaction. The method is less commonly used relative to other cross-coupling methods in part due to lack of availability of organozinc species. While organozinc species can be prepared, problems with reproducibility and handling of these sensitive species can complicate these reactions. Herein, we describe the continuous formation, using an activated packed-bed of metallic zinc, and subsequent use of organozinc halides. We demonstrate that a single column of zinc can provide excellent yields of organozinc halides and that they can be used downstream in subsequent Negishi cross-couplings. The preparation of the zinc column and the scope of the reaction are discussed.
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