Chemoselective and Kilogram-scale Synthesis of Acetanilide β3-Adrenergic Receptor Agonist

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概要

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• We describe an alternative route for the synthesis of β3-adrenergic receptor agonist (S)-2- (2-phenyl-amino-1,3-thiazol-4-yl)-4'-{2-[(2-hydroxy-3-phenoxypropyl)amino]ethyl}acetanilide (1). The key intermediate (S)-1-{[2-(4-aminophenyl)ethyl]amino}-3-phenoxypropan-2-ol monohydro- chloride (2) was condensed with 2-(2-phenylamino-1,3-thiazol-4-yl)acetic acid (3) using 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide hydrochloride (EDCI·HCl) to give 1 as a product of chemoselective amide formation on the aromatic amine moiety. This synthetic route was successfully applied to kilogram-scale preparation without purification via chromatography.

• 公益社団法人 日本化学会の論文

著者

• Sugimori Toshiyuki

  Process Chemistry Labs, Astellas Pharma Inc.

• Kawazoe Souichirou

  Process Chemistry Labs, Astellas Pharma Inc.

• Suzuki Takayuki

  Medicinal Chemistry Research Labs, Astellas Pharma Inc.

• Nakamura Hirofumi

  Process Chemistry Labs, Astellas Pharma Inc.

• Onda Kenichi

  Medicinal Chemistry Research Labs, Astellas Pharma Inc.

• Maruyama Tatsuya

  Medicinal Chemistry Research Labs, Astellas Pharma Inc.

• Okada Minoru

  Process Chemistry Labs, Astellas Pharma Inc.

関連論文

• Chemoselective and Kilogram-scale Synthesis of Acetanilide β3-Adrenergic Receptor Agonist

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