Fischer, H. et al. published their research in Justus Liebigs Annalen der Chemie in 1926 |CAS: 89909-51-3

4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde(cas:89909-51-3) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. Formula: C7H8BrNO

Fischer, H.; Ernst, Paul published an article in 1926, the title of the article was Halogen-substituted pyrroles. IV. New preparation of pyrrole-α-aldehydes and stable tripyrrylmethanes.Formula: C7H8BrNO And the article contains the following content:

2,4-Dimethyl-5-carbethoxypyrrole and Br in CCl4 give nearly quant. the 3-Br derivative (IV), m. 150°, which, on further bromination, gives 85% of 2-bromomethyl-3-bromo-4-methyl-5-carbethoxypyrrole (V), decomposing 165-7°. The free acid (VI) from IV treated with 3 mols. Br in a little CCl4 gives [2,4-dimethyl-3-bromopyrryl][2,4-dibromo-3-methylpyrryl]methene, dark red, m. 192°. VI (5 g.), through the Gattermann aldehyde synthesis, gives 1 g. 2,4-dimethyl-3-bromo-5-formylpyrrole (VII), m. 166-7° (decomposition) (phenylhydrazone, decomposes 99-100°; semicarbazone, m. 223-4° (decomposition)). VII, warmed with EtOH-HCl, gives bis-[2,4-dimethyl-3-bromopyrrole-5]-methene, decomposes 187°. All attempts to prepare the corresponding alc. from V by heating with H2O failed. With AcOK there results quant. 2-acetoxymethyl-3-bromo-4-methyl-5-carbethoxypyrrole, m. 107-9°; the Ehrlich reaction is negative. The corresponding 2-chloroacetoxymethyl derivative, m. 150-3°, decomposes 172°; the 2-formoxymethyl derivative, m. 146-8° (decomposition). 2-Anilinomethyl derivative, m. 128-9° (50-60% yield); dehydration with KMnO4 in Me2CO-H2O gives 70% of the Schiff base, C15H15O2N2Br, m. 127-8°, which is catalytically reduced to the anilide and adds HCl, giving the compound C15H16O2N2BrCl, decomposes 216°. In boiling H2O containing the calculated amount of HCl, the base gives 70% of 2-carbethoxy-3-methyl-4-bromo-5-formylpyrrole (VIII), m. 134-6° (phenylhydrazone, m. 144°; oxime, m. 155-6°; semicarbazone, decomposes 260°). The free acid has no characteristic decomposition point, gives a positive Ehrlich reaction in the hot and on boiling with concentrated HCl gives a violet-red color. The Schiff base, C13H20O4N2, m. 82°, from 2-anilinomethyl-4-methyl-3,5-dicarbethoxypyrrole, gives 2-formyl-4-methyl-3,5-dicarbethoxypyrrole (IX), m. 124°; 1 l. boiling H2O dissolves 0.65 g.; it reduces NH4OH-AgNO3 but not Fehling solution; 1 g. in EtONa (1 g. Na and 10 cc. EtOH) gives 2-formyl-3-carbethoxy-4-methyl-5-pyrrolecarboxylic acid, decomposing 195°; 1 l. boiling H2O dissolves 6.5 g. Excess alkali gives 2-formyl-4-methylpyrrole-3,5-dicarboxylic acid, does not decompose at 250°. 2-Anilinomethyl-3-carbethoxy-4-methyl-5-pyrrolecarboxylic acid, decomposes 186°; dry distillation gives a non-crystalline oil, giving positive PhNH2 and Ehrlich aldehyde reactions. 2-Anilinomethyl-3-bromo-4-methyl-5-pyrrolecarboxylic acid, decomposes 197°. IX and 2,4-dimethyl-3-carbethoxypyrrole give [bis-(2,4-dimethyl-3-carbethoxy)]-3,5-dicarbethoxy-4-methylpyrryl-2-methane, m. 179°. The corresponding 3-Ac derivative, m. 254-5° the 5-carbethoxy derivative, m. 109-200°. VIII gives [bis-(2,4-dimethyl-3-carbethoxy)]-3-bromo-4-methyl-5-carbethoxypyrryl-2-methane, m. 227-8°. They readily take up EtOH of crystallization and are best crystallized from H2O. The AcOH solution gives a deep red color with K2Cr2O7 but does not show an absorption spectrum. Ehrlich’s reagent in the hot gives a positive reaction but is accompanied by a hydrolysis; they are stable towards concentrated HCl. Catalytic reduction of IX gives 2-hydroxymethyl-3,5-dicarbethoxy-4-methylpyrrole, m. 116°; Ac derivative, m. 113°; CrO3 oxidizes it to IX. HBr gives the 2-bromomethyl derivative, m. 156°. Upon heating, HCHO is slowly evolved with the formation of II’. Heating with pyrroles gives the corresponding methanes. 2,4-Dimethyl-3-ethyl-5-carbethoxypyrrole and Br in AcOH at 35-40° give about 75% of the 2-bromomethyl derivative, m. 132-4° (decomposition); 2-anilinomethyl derivative, m. 144-5° (40-50% yield); the Schiff base, C17H20O2N2, yellow, m. 133°; the HCl addition product, light yellow, m. 196° (decomposition); with aqueous AcONa there results a compound, m. 119-20°; boiling with a large amount of H2O gives 90% of 2-formyl-3-ethyl-4-methyl-5-carbethoxypyrrole, m. 90°; 500 g. hot H2O dissolves about 0.2 g.; oxime, m. 150°. With 2 mols. 2,4-dimethyl-3-carbethoxypyrrole in EtOH-HCl there results the HCl salt of the methene. The experimental process involved the reaction of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde(cas: 89909-51-3).Formula: C7H8BrNO

4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde(cas:89909-51-3) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. Formula: C7H8BrNO

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Bouerat, Laeetitia et al. published their research in Journal of Medicinal Chemistry in 2005 |CAS: 89909-51-3

The Article related to indolinone multiple sclerosis sar preparation derivative antiinflammatory, Pharmacology: Structure-Activity and other aspects.Product Details of 89909-51-3

On August 25, 2005, Bouerat, Laeetitia; Fensholdt, Jef; Liang, Xifu; Havez, Sophie; Nielsen, Simon F.; Hansen, Jens R.; Bolvig, Simon; Andersson, Christina published an article.Product Details of 89909-51-3 The title of the article was Indolin-2-ones with High in Vivo Efficacy in a Model for Multiple Sclerosis. And the article contained the following:

The known KDR inhibitor SU5416 and several analogs of the indolin-2-one family were surprisingly found to be highly efficacious in the EAE model, an established model for multiple sclerosis. The high in vivo effect could be correlated to in vitro inhibition of the pro-inflammatory cytokine IL-2. Activity following po administration was obtained with several analogs and via the use of prodrugs. The experimental process involved the reaction of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde(cas: 89909-51-3).Product Details of 89909-51-3

The Article related to indolinone multiple sclerosis sar preparation derivative antiinflammatory, Pharmacology: Structure-Activity and other aspects.Product Details of 89909-51-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Kancharla, Papireddy et al. published their patent in 2016 |CAS: 89909-51-3

The Article related to antimalarial tambjamine prodiginine preparation sar, Alkaloids: Alkaloids Containing Three Or More Nitrogen Atoms and other aspects.HPLC of Formula: 89909-51-3

On November 3, 2016, Kancharla, Papireddy; Kelly, Jane Xu; Reynolds, Kevin A. published a patent.HPLC of Formula: 89909-51-3 The title of the patent was Preparation of tambjamines and B-ring functionalized prodiginines as potent antimalarials. And the patent contained the following:

The invention is related to compounds I [(i) R1 is H, lower alkyl or lower alkoxy; R2 is H, lower alkyl, lower alkoxy, halo, or pyrrolyl; R3 is aryl or heteroaryl; and R4 is cycloalkyl; or (ii) R1-3 independently are lower alkyl; and R4 is alkyl or cycloalkyl] and II and their pharmaceutically acceptable salts. Specifically, the synthesis and antimalarial activity of 94 novel bipyrrole tambjamines (TAs) and a library of B-ring functionalized tripyrrole prodiginines (PGs) against a panel of Plasmodium falciparum strains are described. The activity and structure-activity relationships demonstrate that the ring-C of PGs can be replaced by an alkylamine, providing for TAs with retained/enhanced potency. Furthermore, ring-B of PGs/TAs can be substituted with short alkyl substitutions at either 4-position (replacement of OMe) or 3- and 4-positions without impacting potency. Eight representative TAs and two PGs have been evaluated for antimalarial activity against multidrug-resistant P. yoelii in mice in the dose range of 5-100 mg/kg × 4 days by oral administration. The KAR425 TA (III) offered greater efficacy than previously observed for any PG, providing 100% protection to malaria-infected mice until day 28 at doses of 25 and 50 mg/kg × 4 days, and was also curative in this model in a single oral dose (80 mg/kg). III was tested using the Ames assay at concentration of 10 uM, with and without S9 activation, against Salmonella typhimurium TA1OO and TA98, there was no increase over the background reversion rate demonstrating its non-genotoxic character. The experimental process involved the reaction of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde(cas: 89909-51-3).HPLC of Formula: 89909-51-3

The Article related to antimalarial tambjamine prodiginine preparation sar, Alkaloids: Alkaloids Containing Three Or More Nitrogen Atoms and other aspects.HPLC of Formula: 89909-51-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Kancharla, Papireddy et al. published their research in Journal of Medicinal Chemistry in 2015 |CAS: 89909-51-3

The Article related to antimalarial tambjamine prodiginine preparation sar, Alkaloids: Alkaloids Containing Three Or More Nitrogen Atoms and other aspects.Application In Synthesis of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde

On September 24, 2015, Kancharla, Papireddy; Kelly, Jane Xu; Reynolds, Kevin A. published an article.Application In Synthesis of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde The title of the article was Synthesis and Structure-Activity Relationships of Tambjamines and B-Ring Functionalized Prodiginines as Potent Antimalarials. And the article contained the following:

Synthesis and antimalarial activity of 94 novel bipyrrole tambjamines (TAs) and a library of B-ring functionalized tripyrrole prodiginines (PGs) against a panel of Plasmodium falciparum strains are described. The activity and structure-activity relationships demonstrate that the ring-C of PGs can be replaced by an alkylamine, providing for TAs with retained/enhanced potency. Furthermore, ring-B of PGs/TAs can be substituted with short alkyl substitutions at either 4-position (replacement of OMe) or 3- and 4-positions without impacting potency. Eight representative TAs and two PGs have been evaluated for antimalarial activity against multidrug-resistant P. yoelii in mice in the dose range of 5-100 mg/kg × 4 days by oral administration. The KAR425 TA (I) offered greater efficacy than previously observed for any PG, providing 100% protection to malaria-infected mice until day 28 at doses of 25 and 50 mg/kg × 4 days, and was also curative in this model in a single oral dose (80 mg/kg). This study presents the first account of antimalarial activity in tambjamines. The experimental process involved the reaction of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde(cas: 89909-51-3).Application In Synthesis of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde

The Article related to antimalarial tambjamine prodiginine preparation sar, Alkaloids: Alkaloids Containing Three Or More Nitrogen Atoms and other aspects.Application In Synthesis of 4-Bromo-3,5-dimethyl-1H-pyrrole-2-carbaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary