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Polymer-Supported Organotin Reagents: Toward an Efficient and Green Route for the preparation of Heterocycles – PSOR

Submission summary

Tetrazoles (RCN4H) are often used as metabolism-resistant isosteric replacements for carboxylic acids (RCO2H) in medicinal chemistry. One of the most efficient preparations of these heterocycles involves organotin azide which induces the presence of tin byproducts difficult to eliminate and exhibiting some toxicity. Since the tin contamination in a biological active compound is proscribed, the use of the synthetic route is compromised. To date, only partition methods have been proposed to solve partially this problem in spite of the importance of tetrazoles in medicinal chemistry. In the present research program, we propose to develop a methodology using polymer-supported organotin reagents to achieve an efficient and clean preparation of tetrazoles. ...

Project coordination

Erwan LE GROGNEC (Organisme de recherche)

The author of this summary is the project coordinator, who is responsible for the content of this summary. The ANR declines any responsibility as for its contents.

Partner

Help of the ANR 150,000 euros
Beginning and duration of the scientific project: - 24 Months

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