- NOVEL MACROCYCLIC DERIVATIVES, PROCESS FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
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Compound of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, X, Y and G are as defined in the description, and their use in the manufacture of medicaments.
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Paragraph 0360; 0361
(2020/08/25)
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- An enantioselective synthesis of α-alkylated pyrroles: Via cooperative isothiourea/palladium catalysis
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Herein we describe the direct enantioselective Lewis base/Pd catalysed α-allylation of pyrrole acetic acid esters. This provides high isolated yields of highly enantioenriched products and exhibits broad reaction scope with respect to both reaction partners. The products can be readily elaborated in a manner which points towards potential applications in target directed synthesis.
- Rush Scaggs,Scaggs, Toya D.,Snaddon, Thomas N.
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supporting information
p. 1787 - 1790
(2019/02/20)
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- Synthesis, antimicrobial, and anti-inflammatory activities of acetamido pyrrolyl azoles
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The acetamido pyrrolyl oxazoles/thiazoles/imidazoles were prepared and tested for their antimicrobial and anti-inflammatory activities. The nitro substituted acetamido pyrrolyl thiazole (11f) and pyrrolyl imidazole (12f) exhibited promising antibacterial activity against K. pneumoniae. The compound 12f showed good antifungal activity against P. chrysogenum. The methoxy acetamido pyrrolyl oxazole (10c) displayed potential anti-inflammatory activity.
- Sowmya, Donthamsetty V.,Basha, Shaik Sharafuddin,Devi, Palampalli Uma Maheswari,Lavanyalatha, Yerraguravagari,Padmaja, Adivireddy,Padmavathi, Venkatapuram
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p. 1010 - 1021
(2017/04/13)
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- Synthesis and process optimization of amtolmetin: An antiinflammatory agent
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Efforts toward the synthesis and process optimization of amtolmetin guacil 1 are described. High-yielding electrophilic substitution followed by Wolf-Kishner reduction are the key features in the novel synthesis of tolmetin 2 which is an advanced intermediate of 1.
- Reddy, Lekkala Amarnath,Chakraborty, Saurya,Swapna, Rodda,Bhalerao, Dinesh,Malakondaiah, Golla China,Ravikumar, Mylavarapu,Kumar, Abhijeet,Reddy, Gade Srinivas,Naram, Jyothirmayi,Dwivedi, Namrata,Roy, Arnab,Himabindu, Vurimidi,Babu, Bangaru,Bhattacharya, Apurba,Bandichhor, Rakeshwar
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scheme or table
p. 362 - 368
(2011/03/21)
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- Friedel - Crafts acylation of pyrroles and indoles using 1,5-diazabicyclo[4.3.0]non-5-ene (DBN) as a nucleophilic catalyst
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1,5-Diazabicyclo[4.3.0]non-5-ene (DBN) has been shown to be an effective catalyst for the regioselective Friedel - Crafts C-acylation of pyrroles and indoles in high yields. A detailed mechanistic study implies that DBN is acting as a nucleophilic organocatalyst, with the X-ray crystal structure of a key N-acyl-amidine intermediate having been determined for the first time.
- Taylor, James E.,Jones, Matthew D.,Williams, Jonathan M. J.,Bull, Steven D.
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supporting information; experimental part
p. 5740 - 5743
(2011/03/18)
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- Rhodium(II) catalyzed intramolecular insertion of carbenoids derived from 2-pyrrolyl and 3-indolyl α-diazo-β-ketoesters and α-diazoketones
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α-Diazo-β-ketoesters and α-diazoketones derived from 2-pyrrolylacetic, 2-pyrrolylpropionic, 3-indolylacetic and 3-indolylpropionic acids afforded carbenoid derived cyclization products on treatment with catalytic rhodium(II) acetate.
- Cuevas-Ya?ez, Erick,Muchowski, Joseph M.,Cruz-Almanza, Raymundo
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p. 1505 - 1511
(2007/10/03)
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- Triazolo(pyrrolo, thieno or furano)azepine derivatives
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Antiallergic triazolo(pyrrolo, thieno or furano)azepines of formula STR1 the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; -E-G- is a bivalent radical of formula X represents O, S or NR3 ; R3 represents hydrogen, C1-6 alkyl or C1-4 alkylcarbonyl; -B=D- is a bivalent radical of formula L represents hydrogen; C1-6 alkyl; substituted C1-6 alkyl; C3-6 alkenyl; C3-6 alkenyl substituted with aryl; or, L represents a radical of formula -Alk-Y-Het1 (c-1), -Alk-NH--CO-Het2 (c-2) or -Alk-Het3 (c-3). Compositions comprising said compounds, processes of preparing the same and intermediates in the preparation thereof.
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- Process for preparing pyrrole-2-acetic acids
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N-H and N-loweralkyl pyrrole-2-acetic acids are prepared by the reduction of 1-H and 1-loweralkyl-α-trichloromethylpyrrole-2-methanol with sodium dithionite (sodium hydrosulfite) in the presence of a base, MOH, wherein M is an alkali metal, an alkaline earth metal or tetraalkyl ammonium.
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- Preparation of pyrrole-2-acetic acid derivatives
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Catalytic dehydrogenation of Δ-2,α-pyrrolidenemalonates and Δ-2,α-pyrrolidenemalononitriles yields pyrrole-2-acetates and pyrrole-2-acetonitriles, respectively. Subsequent hydrolysis of the latter affords pyrrole-2-acetic acids.
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