Syntheses of 3-Substituted Pyrrole Derivatives with Antiinflammatory Activity

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概要

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• Various dimethyl 3-substituted pyrrole-2,4-dicarboxylates (3) were synthesized by the reaction of methyl isocyanoacetate (2) with methyl α-isocyanoacrylates (5) in the presence of base. This type of reaction was also applicable to the preparation of 3-substituted pyrrole-2,4-dicarboxamides (10) by employing appropriate amide compounds (8) or (9) and (12) as reactants. Hydrolysis followed by decarboxylation of the pyrrole diester compounds (3) gave 3-substituted pyrroles (14) in good yields. A series of these compounds (14) showed antiinflammatory activities against carrageenan-induced rat paw edema. Among the compounds tested, 3-(2-chlorophenyl) pyrrole (14d) was found to be more potent than mefenamic acid.

• 1980-08-25

著者

• 鈴木 護

  Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd.,

• 沼波 憲一

  生化研

• 岩澤 義郎

  Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.,

• 岩澤 義郎

  Pharmacological Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 米田 直人

  Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd.

• 小野田 有一

  Biological Research Laboratory, Tanabe Seiyaku Co,. Ltd.

• 米田 直人

  Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd.

• 岩澤 義郎

  Biological Research Laboratory Tanabe Seiyaku Co. Ltd.

• 鈴木 護

  Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd.

• 坂井 和夫

  Research Laboratory of Applied Biochemistry Tanabe Seiyaku Co., Ltd.

• 坂井 和夫

  Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd.

• 小野田 有一

  Biological Research Laboratory Tanabe Seiyaku Co . Ltd.

• 米田 直人

  Research Laboratory of Applied Biochemistry

• 米田 直人

  Research Laboratory of Applied Biochemistry Tanabe Seiyaku Co., Ltd.

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