2-Oxo-1,2-ethylenedioxy group as a linker for solution-, liquid-, and solid-phase syntheses to discover drug-like small molecules

Masato Oikawa; Yoshiyuki Takeda; Makoto Sasaki

doi:10.1016/j.tetlet.2005.04.138

2-Oxo-1,2-ethylenedioxy group as a linker for solution-, liquid-, and solid-phase syntheses to discover drug-like small molecules

Masato Oikawa, Yoshiyuki Takeda, Makoto Sasaki

LIF - Molecular and Chemical Life Science

Research output: Contribution to journal › Article › peer-review

5 Citations (Scopus)

Abstract

2-Oxo-1,2-ethylenedioxy (2-OED) functionality has been prepared on a soluble MPEG polymer and solid (HM resin and Lanterns) supports as platforms for discovery of drug-like small molecules. The functionality is cleaved either by Yb(OTf)₃ or TMSCHN₂ in MeOH, or by various amines to release small molecules synthesized on the platform in good yield. Application of these platforms aiming for discovery of potent agonists for growth hormone secretagogue is reported by using the Ugi four-component coupling reaction.

Original language	English
Pages (from-to)	4667-4670
Number of pages	4
Journal	Tetrahedron Letters
Volume	46
Issue number	27
DOIs	https://doi.org/10.1016/j.tetlet.2005.04.138
Publication status	Published - 2005 Jul 4

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

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10.1016/j.tetlet.2005.04.138

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AU - Oikawa, Masato

AU - Takeda, Yoshiyuki

AU - Sasaki, Makoto

PY - 2005/7/4

Y1 - 2005/7/4

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AB - 2-Oxo-1,2-ethylenedioxy (2-OED) functionality has been prepared on a soluble MPEG polymer and solid (HM resin and Lanterns) supports as platforms for discovery of drug-like small molecules. The functionality is cleaved either by Yb(OTf)3 or TMSCHN2 in MeOH, or by various amines to release small molecules synthesized on the platform in good yield. Application of these platforms aiming for discovery of potent agonists for growth hormone secretagogue is reported by using the Ugi four-component coupling reaction.

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JO - Tetrahedron Letters

JF - Tetrahedron Letters

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ER -

2-Oxo-1,2-ethylenedioxy group as a linker for solution-, liquid-, and solid-phase syntheses to discover drug-like small molecules

Abstract

ASJC Scopus subject areas

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