104384-69-2Relevant articles and documents
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.
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.
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)