Suggestions
Subrata Shaw
Senior Principal Scientist @ Pfizer | Drug Discovery
Subrata Shaw, a highly experienced synthetic and medicinal chemist, has an extensive background in early-stage target validation, hit discovery, optimization, and lead optimization efforts that result in clinical candidates. He specializes in organic synthesis, medicinal chemistry, and fragment-based drug discovery, and excels at designing and synthesizing analogs to optimize potency, physical properties, and ADME characteristics of lead molecules. He has an exceptional talent for analyzing data, strategic planning, and executing tactics. Shaw's educational background includes a Doctor of Philosophy (PhD) in Organic Chemistry from Oregon State University, an M.S in Chemistry from Indian Institute of Technology, Kanpur, and a B.S. in Chemistry from Calcutta University.
With an impressive career, Shaw has worked across numerous organizations ranging from Broad Institute of MIT and Harvard as a Research Scientist II, Vanderbilt University Medical Center as a BRET Postdoctoral Fellow, and Oregon Translational Research & Development Institute as a Collaborative Research Assistant. Notably, he has also held positions as a Doctoral Researcher and Teaching Assistant at Oregon State University and as a Summer Research Intern at McMaster University. Beyond his academic credentials and professional experience, Shaw has authored numerous publications in scientific journals.
Shaw's unique blend of scientific expertise and strategic thinking make him a valuable asset to any organization looking to develop new drugs.
Highlights
Excellent work from Merck/Sarpong/Sigman lab demonstrating 14N→15N isotopic exchange/transmutation of nitrogen heteroaromatics through skeletal editing in a one-step procedure through the triflylation of a nitrogen atom, followed by a ring-opening/ring-closure sequence mediated by 15N-aspartate to effect isotopic exchange of the nitrogen atom (much like the Zincke reaction). Key to the success of this transformation is the formation of an isolable 15N-succinyl intermediate, which undergoes elimination to give the isotopically labeled heterocycle.
The reaction happens under mild conditions providing high isotopic yields which makes it very useful for synthesis N15-labelled recombinant proteins (e.g. for NMR-based Fragment Screening) as well as for tracing metabolism in LO. #Isotopic_Labeling #Late_Stage_Functionalization https://lnkd.in/e-BhDPMU
Even though amide coupling may not be the reaction that could keep a medicinal chemist up at night, I do feel this novel amide formation methodology employing isocyanides as nucleophiles in SN2 reactions with alkyl halides and concomitant in situ hydrolysis of the intermediate nitrilium ion represents a unique methodology which harnesses orthogonal reactivity of the two reagents for the amide formation compared to the classical carboxylic acid & amines.
This methodology could be very valuable in bioconjugation chemistry (involving e.g. aspartate, glutamate, serine, threonine or even lysine) if the transformation can be done in ‘milder’ conditions in future. #MCR #Bioconjugation #MedChem
https://lnkd.in/egDVVrDG
