Synthesis of Metabolites of S-1452,an Orally Active Thromboxane A_2 Receptor Antagonist

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概要

• 論文の詳細を見る

• The synthesis of 16 metabolites of S-1452,an orally active thromboxane A_2 (TXA_2) receptor antagonist, is described. Regioselective hydroxylation at C-5 or C-6 of the bicyclo[2.2.1]heptane skeleton of the optically active intermediate 16 was attempted by using 9-borabicyclo[3.3.1]nonane followed by H_2O_2 or m-chloroperbenzoic acid (m-CPBA) and then LiAlH_4,to obtain the hydroxylated product 17a or 17b, respectively. Modification of the C-2 substituent of 17a and 17b afforded eight metabolites of S-1452. Eight non-hydroxylated metabolites were synthesized by using a similar reaction sequence.

• 社団法人日本薬学会の論文
• 1991-11-25

著者

• 渡辺 文彦

  Shionogi Research Laboratories Shionogi & Co. Ltd.

• 松浦 孝治

  Shionogi Research Laboratories, Shionogi & Co., Ltd.,

• 白波瀬 和裕

  Shionogi Research Laboratories, Shionogi & Co., Ltd.,

• 大谷 光昭

  Shionogi Research Laboratories, Shionogi & Co., Ltd.,

• 白波瀬 和裕

  Shionogi Research Laboratories Shionogi & Co. Ltd.

• 大谷 光昭

  Shionogi Research Laboratories Shionogi & Co. Ltd.

• 松浦 孝治

  Shionogi Research Laboratories Shionogi & Co. Ltd.

関連論文

• Synthesis of Metabolites of S-1452,an Orally Active Thromboxane A_2 Receptor Antagonist
• The C-1,2 Isomeric Ketols and Diols in 17β-Hydroxy-A-nor-5α-androstane Series
• Syntheses of 1α, 2α-and 1β, 2β-Epithio-A-nor-5α-androstan-17β-ol and Related Compounds.
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• The Substituent Effect on the Addition Course of the Diels-Alder Reaction of 2-Methyl-5-substituted-1,4-benzoquinones with Butadiene

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