Issue 1, 2013
From the journal:

MedChemComm

On the importance of synthetic organic chemistry in drug discovery: reflections on the discovery of antidiabetic agent ertugliflozin†‡§

Vincent Mascitti,*a   Benjamin A. Thuma,a   Aaron C. Smith,a   Ralph P. Robinson,a   Thomas Brandt,a   Amit S. Kalgutkar,a   Tristan S. Maurer,a   Brian Samasa  and  Raman Sharmaa  

* Corresponding authors

a Pfizer Global Research & Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, USA
E-mail: vincent.mascitti@pfizer.com
Fax: +1 845 474 5876
Tel: +1 860 686 3455

Abstract

The discovery of antidiabetic agent ertugliflozin is described. The compound belongs to a new class of SGLT2 inhibitors bearing a dioxa-bicyclo[3.2.1]octane motif. This article describes the critical role that organic synthesis played in both influencing our medicinal chemistry strategy and speeding up the progression of our program.

Graphical abstract: On the importance of synthetic organic chemistry in drug discovery: reflections on the discovery of antidiabetic agent ertugliflozin

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Article information

DOI
https://doi.org/10.1039/C2MD20163A
Article type
Concise Article
Submitted
24 Jun 2012
Accepted
11 Jul 2012
First published
16 Jul 2012

Med. Chem. Commun., 2013,4, 101-111

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On the importance of synthetic organic chemistry in drug discovery: reflections on the discovery of antidiabetic agent ertugliflozin

V. Mascitti, B. A. Thuma, A. C. Smith, R. P. Robinson, T. Brandt, A. S. Kalgutkar, T. S. Maurer, B. Samas and R. Sharma, Med. Chem. Commun., 2013, 4, 101 DOI: 10.1039/C2MD20163A

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