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Issue 1, 2013
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On the importance of synthetic organic chemistry in drug discovery: reflections on the discovery of antidiabetic agent ertugliflozin§

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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


Submitted
24 Jun 2012
Accepted
11 Jul 2012
First published
16 Jul 2012

Med. Chem. Commun., 2013,4, 101-111
Article type
Concise Article

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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