Chemical Synthesis of the ODM-201’s Diastereomers through an Efficient Intramolecular 1,3-Dipolar Cycloaddition

Tingting Pan; Chunguang Xia; Huijuan Jiang; Zhongtang Zhang; Xueyan Zhu; Yulei Yang

doi:10.1248/cpb.c17-00176

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Chemical Synthesis of the ODM-201’s Diastereomers through an Efficient Intramolecular 1,3-Dipolar Cycloaddition

Tingting Pan, Chunguang Xia, Huijuan Jiang, Zhongtang Zhang, Xueyan Zhu, Yulei Yang

著者情報

キーワード: ODM-201, diastereomers, synthesis, intramolecular 1,3-dipolar cycloaddition

ジャーナルフリー早期公開

論文ID: c17-00176

DOI https://doi.org/10.1248/cpb.c17-00176

この記事には本公開記事があります。

The final version of this article is now available: Vol. 65 (2017), No. 6 pp. 582-585

詳細

抄録

An efficient synthesis of ODM-201’s diastereomers has been developed from (R)-methyl 3-hydroxybutanoate or (S)-methyl 3-hydroxybutanoate, respectively, with high overall yield and excellent diastereomeric purity. The key step in this synthesis is the preparation of the key intermediate (R)-5-(1-((tert-butyldimethylsilyl)oxy)ethyl)-1H-pyrazole-3-carboxylic acid or (S)-5-(1-((tert-butyldimethylsilyl)oxy)ethyl)-1H-pyrazole-3-carboxylic acid through intramolecular 1,3-dipolar cycloaddition of the vinyl diazo carbonyl compounds.

責任著者(Corresponding author)

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