Tetrahedron Letters p. 3651 - 3654 (1999)
Update date:2022-07-30
Topics:
Hansen, Thomas K.
Schlienger, Nathalie
Hansen, Birgit S.
Andersen, Peter H.
Bryce, Martin R.
The focus of this paper is the chemistry of 2-piperazinones and the use of this building block to restrict the conformational freedom of the growth hormone secretagogue NN703 (currently in clinical development). We exploit classical methods for 2-piperazinone synthesis as well as some novel approaches such as a Boronic Mannich reaction. Finally, we report on the ability of the constrained target compounds to release growth hormone in vitro.
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