- METHOD FOR PRODUCING PYRROLE DERIVATIVE, AND INTERMEDIATE THEREOF
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The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [wherein R1 represents a C1-C4 alkyl group, and R2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate.
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Paragraph 0187
(2016/09/12)
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- CRYSTAL OF PYRROLE DERIVATIVE AND METHOD FOR PRODUCING THE SAME
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The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.
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- ATROPISOMER OF PYRROLE DERIVATIVE
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[Object] A prophylactic or therapeutic agent for a cardiovascular disease is provided. [Means for Resolution] An atropisomer of a compound represented by the following general formula (I): (wherein R1 is a C1-C3 alkyl group or a hydroxy-C1-C3 a
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