104384-69-2Relevant academic research and scientific papers
Diminished reactivity of ortho-substituted phenacyl bromides toward nucleophilic displacement
Kalendra, Diane M.,Sickles, Barry R.
, p. 1594 - 1596 (2003)
A systematic increase of substitution rates by tert-butylamine on α-bromopropiophenones is observed with meta or para substituents with increasing electron-withdrawing ability (k x 103 L M-1 min-1 = 12.7 (p-CH3), 15.7 (o-F), 20.5 (H), 20.0 (p-Cl), 23.6 (m-Cl), 27.3 (p-CF3)). Within an ortho-substituted series, the reactivities decrease (k x 103 L M-1 min-1 = 7.64 (o-OCH3), 5.31 (o-CH3), 2.85 (o-Cl), 2.40 (o-CF3)). Ortho-substitution results occur from rotational barrier effects and an Aδσ + Bδσ + repulsion. The major bonding contribution between reaction and α-substituent centers (A-B) is only the σ bond. When π bonding is allowed between A and B (meta/para-substitution), delocalization and stabilization of the reacting center occurs.
CRYSTAL OF PYRROLE DERIVATIVE AND METHOD FOR PRODUCING THE SAME
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Paragraph 0121; 0122; 0123, (2016/05/02)
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.
Method for producing pyrrole derivative, and intermediate thereof
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Paragraph 0093, (2016/10/09)
The present invention provides a method for producing an atropisomer of a pyrrole derivative having an exceptional mineralocorticoid receptor antagonizing effect, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [in the formula, R1 indicates a C1-C4 alkyl group, and R2 indicates a 2-hydroxyethyl group or carboxymethyl group] as a production intermediate.
METHOD FOR PRODUCING PYRROLE DERIVATIVE, AND INTERMEDIATE THEREOF
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Paragraph 0134-0136, (2016/09/12)
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.
DIPYRROMETHENE CRYSTAL AND METHOD FOR MANUFACTURING SAME
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Paragraph 0174-0177, (2016/11/14)
The present invention refers to mineral excellent pyrrole derivatives having an antagonistic effect on receptor [...] atropisomers of intermediates for preparations of the same, provides concentration and recording medium storing record manufacturing method. 5beta eggs skeleton and optically active amines, which over a long period of time, characterized by, the general formula (I) [In formula, R 1 the methyl or trifluoromethyl indicates the, R 2 hydrogen atom, alkyl having C1-C3 alkoxy groups indicates the, n the exhibits is an integer selected from 1 ~ 3] atropisomers of including process and method for splitting, and manufacturing method isomers atropisomers of pyrrole derivatives (S)-1-(2-hydroxyethyl)-4-methyl-N-[ 4-(methylsulfonyl) phenyl]-5-[ 2-(trifluoromethyl) phenyl]-1H-pyrrole-3-carboxamide determination of. (by machine translation)
Therapeutically useful 1-phenyl-2-piperidinoalkanol derivatives
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, (2008/06/13)
Compounds of the formula: STR1 wherein R1 is hydrogen, halogen, trifluoromethyl, alkyl, hydroxyl, alkyoxy, benzyloxy, alkanoyloxy, or benzoyloxy, or when R2 is hydroxyl or methoxy in the 4-position and R3 is hydrogen, R1 may also represent hydroxymethyl carbamoyl or alkoxycarbonyl, R2 is hydrogen, halogen, alkyl, hydroxyl, or alkoxy, R3 is hydrogen or alkyl, R4 is alkyl (in which case the compounds are (±)-erythro) or when R3 represents hydrogen, R4 may also be hydrogen, and R5 is hydrogen, halogen, alkyl, alkoxy, or three methoxy groups in the 3-, 4- and 5-positions and pharmaceutically acceptable acid addition salts thereof, with the exclusion of compounds wherein: (a) one of R1 and R2 is in the 4-position and is hydroxyl, alkoxy or benzyloxy, the other is in the 3-position and is hydrogen, hydroxyl, alkoxy or benzyloxy, and R3 and R5 are hydrogen and wherein: (b) R1 is in the 4-position and is halogen, R4 is methyl and R2, R3 and R5 are hydrogen, are useful as medicaments.
