Tag: 200-300

On October 13, 2021, Kawamata, Yu; Hayashi, Kyohei; Carlson, Ethan; Shaji, Shobin; Waldmann, Dirk; Simmons, Bryan J.; Edwards, Jacob T.; Zapf, Christoph W.; Saito, Masato; Baran, Phil S. published an article.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Chemoselective Electrosynthesis Using Rapid Alternating Polarity. And the article contained the following:

Challenges in the selective manipulation of functional groups (chemoselectivity) in organic synthesis have historically been overcome either by using reagents/catalysts that tunably interact with a substrate or through modification to shield undesired sites of reactivity (protecting groups). Although electrochem. offers precise redox control to achieve unique chemoselectivity, this approach often becomes challenging in the presence of multiple redox-active functionalities. Historically, electrosynthesis has been performed almost solely by using d.c. (DC). In contrast, applying a.c. (AC) has been known to change reaction outcomes considerably on an anal. scale but has rarely been strategically exploited for use in complex preparative organic synthesis. Here we show how a square waveform employed to deliver elec. current-rapid alternating polarity (rAP)-enables control over reaction outcomes in the chemoselective reduction of carbonyl compounds, one of the most widely used reaction manifolds. The reactivity observed cannot be recapitulated using DC electrolysis or chem. reagents. The synthetic value brought by this new method for controlling chemoselectivity is vividly demonstrated in the context of classical reactivity problems such as chiral auxiliary removal and cutting-edge medicinal chem. topics such as the synthesis of PROTACs. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to electrochem chemoselective reduction ketone rapid alternating polarity, Heterocyclic Compounds (One Hetero Atom): General and other aspects.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Athira, Ck; Manikandan, Priyadharshini; Kandasamy, Elango; Ramani, Prasanna published an article in 2019, the title of the article was Ionic liquid mediated synthesis of labeled peptide nucleic acid monomer.Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione And the article contains the following content:

We have designed and synthesized phthalimido labeled peptide nucleic acid (PNA) monomer through N-alkylation of α-amino acid ester with N-bromo ethylphthalimide which was facilitated by using ionic liquids The alkylated product was condensed with nucleobase such as thymine-1-acetic acid to get the target compound The labeled-PNA monomer is a new mol. which bears a marker and can be easily prepared in two steps. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to peptide nucleic acid phthalimido labeled synthesis ionic liquid marker, amino acid ester alkylation bromo ethylphthalimide thymine acetic acid, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 7, 2021, Zhou, Shaofang; Lv, Kang; Fu, Rui; Zhu, Changlei; Bao, Xiaoguang published an article.Synthetic Route of 2567-29-5 The title of the article was Nickel/Photoredox Dual Catalytic Cross-Coupling of Alkyl and Amidyl Radicals to Construct C(sp3)-N Bonds. And the article contained the following:

The construction of C(sp3)-N bonds via direct radical-radical cross-coupling under benign conditions is a desirable but challenging approach. Herein, the cross-coupling of alkyl and amidyl radicals to build aliphatic C-N bonds in a concise, mild, and oxidant-free manner is implemented by nickel/photoredox dual catalysis. In this protocol, the single electron transfer strategy is successfully employed to generate N- and C-centered radicals from sulfonyl azides/azidoformates and alkyltrifluoroborates, resp. The photocatalyst-induced triplet-triplet energy-transfer mechanism, however, might not be applicable to this reaction. The oxidative quenching pathway of the excited photocatalyst (RuII/*RuII/RuIII/RuII) combined with a possible NiI/NiII/NiIII/NiI catalytic cycle is proposed to account for the nickel/photoredox dual-catalyzed C(sp3)-N bond formation based on synergistic exptl. and computational studies. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Synthetic Route of 2567-29-5

The Article related to carbon nitrogen bond formation nickel photoredox dual catalysis, sulfonyl azide azidoformate alkyltrifluoroborate alkyl amidyl radical cross coupling, General Organic Chemistry: Synthetic Methods and other aspects.Synthetic Route of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 2, 2021, Duran-Camacho, Geraldo; Ferguson, Devin M.; Kampf, Jeff W.; Bland, Douglas C.; Sanford, Melanie S. published an article.Recommanded Product: 2567-29-5 The title of the article was Isolable Pyridinium Trifluoromethoxide Salt for Nucleophilic Trifluoromethoxylation. And the article contained the following:

An isolable pyridinium trifluoromethoxide salt is prepared from the reaction of 4-dimethylaminopyridine with the com. available liquid 2,4-dinitro(trifluoromethoxy)benzene. The salt is an effective trifluoromethoxide source for SN2 reactions to form trifluoromethyl ethers. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Recommanded Product: 2567-29-5

The Article related to pyridinium trifluoromethoxide salt preparation trifluoromethoxylation reagent, alkyl halide pyridinium trifluoromethoxide salt trifluoromethoxylation, General Organic Chemistry: Synthetic Methods and other aspects.Recommanded Product: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhang, Jie; Song, Xue; Chen, Zhi-Chao; Du, Wei; Chen, Ying-Chun published an article in 2022, the title of the article was Phosphine-catalysed intermolecular cyclopropanation reaction between benzyl bromides and activated alkenes.Reference of 4-(Bromomethyl)-1,1′-biphenyl And the article contains the following content:

While phosphine-mediated reactions were extensively explored over the past few decades, the catalytic cyclopropanation reaction via a phosphonium ylide pathway has been significantly underdeveloped, and an intermol. version still remains to be disclosed. Presented herein was a catalytic cyclopropanation reaction between readily available benzyl bromides and activated alkenes, such as α-cyano chalcones, through in situ formation of phosphonium ylide intermediates. A spectrum of densely functionalized cyclopropane derivatives was efficiently constructed with excellent diastereoselectivity, which can be further converted to five-membered heterocycles after simple transformations. Moreover, moderate enantioselectivity can be obtained by using a com. available DuPhos catalyst. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Reference of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to aralkyl bromide carbonyl cyanochalcone phosphine catalyst diastereoselective cyclopropanation, carbonyl cyanocyclopropane preparation, General Organic Chemistry: Synthetic Methods and other aspects.Reference of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 17, 2021, Yu, Fei; Li, Chuang; Wang, Chuangye; Zhang, Hongwei; Cao, Zhong-Yan published an article.Reference of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was (1-Selenocyanatoethyl)benzene: A Selenocyanation Reagent for Site-Selective Selenocyanation of Inert Alkyl C(sp3)-H Bonds. And the article contained the following:

A new, simple, yet easily accessible, (1-selenocyanatoethyl)benzene was designed and applied as a SeCN group transfer reagent for selenocyanation of aliphatic C(sp3)-H bonds for the first time. This protocol was featured with mild reaction conditions and wide substrate scope. Control experiments revealed that a radical-group transfer mechanism might be involved. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Reference of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to selenocyanatoalkyl arene preparation regioselective, selenocyanatoethyl benzene fluoro sulfonamide selenocyanation copper catalyst, General Organic Chemistry: Synthetic Methods and other aspects.Reference of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 31, 2021, Sarkar, Anindya; Kankanamalage, Anushka C. Galasiti; Zhang, Qian; Cheng, Heng; Sivaprakasam, Prasanna; Naglich, Joseph; Xie, Chunshan; Gangwar, Sanjeev; Boger, Dale L. published an article.Related Products of 2567-29-5 The title of the article was Synthesis, structure-activity relationship studies and evaluation of a TLR 3/8/9 agonist and its analogues. And the article contained the following:

A comprehensive SAR study of a putative TLR 3/8/9 agonist was conducted. Despite the excitement surrounding the potential of the first small mol. TLR3 agonist with a compound that addnl. displayed agonist activity for TLR8 and TLR9, compound I displayed disappointing activity in our hands, failing to match the potency (EC50) reported and displaying only a low efficacy for the extent of stimulated NF-κB activation and release. The evaluation of >75 analogs of I, many of which constitute minor modifications in the structure, failed to identify any that displayed significant activity and none that exceeded the modest activity found for I. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Related Products of 2567-29-5

The Article related to synthesis structure activity relationship tlr3 tlr8 tlr9 agonist, sar study, tlr agonists, tlr3 agonist, toll-like receptor (tlr), General Organic Chemistry: Synthetic Methods and other aspects.Related Products of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 14, 2021, Garofalo, Albert W.; De Lombaert, Stephane; Schwarz, Jacob Bradley; Andreotti, Daniele; Sabbatini, Fabio Maria; Serra, Elena; Bernardi, Silvia; Migliore, Marco; Budassi, Federica; Beato, Claudia published a patent.Related Products of 1427433-22-4 The title of the patent was Indazoles and azaindazoles as LRRK2 inhibitors in the treatment of CNS disorders and their preparation. And the patent contained the following:

The invention relates compounds of formula I, their preparation and their use as inhibitors of LRRK2 in the treatment of CNS disorders. Compound I, wherein A is halo, (un)subsititued C1-6 alkyl, (un)subsititued C2-6 alkenyl, etc.; ring B is Ph and 5- to 10-membered heteroaryl wherein said 5- to 10-membered heteroaryl comprises 1, 2 and 3 ring-forming heteroatoms independently864 selected from N, O and S; X2 is N and CR2; X3 is N and CR3; X4 is N and CR4; no more than two of X2, X3 and X4 are simultaneously N; R1 is independently H, halo, C1-6 alkyl, etc.; R2 and R4 are independently H, halo, C2-6 alkenyl, etc.; R3 is H, halo, C1-6 haloalkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Compound II was prepared by reacting 3-bromo-1H-indazol-5-amine with 3-furanylboronic acid yielding 3-(furan-3-yl)-1H-indazole-5-amine, then 5-cyano-3-fluoropyridine-2-carboxylic acid underwent amidation with 3-(furan-3-yl)-1H-indazole-5-amine to yield compound II. Compound II was evaluated for LRRK2 inhibitory activity resulting in a wild type LRRK2 and G2019S LRRK2 IC50 of ≤ 100 nM for both. Compounds of the invention were evaluated for their LRRK2 inhibitory activity (data given). The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methyl-benzoic acid(cas: 1427433-22-4).Related Products of 1427433-22-4

The Article related to indazole azaindazole preparation lrrk2 inhibitor cns disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 1427433-22-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 9, 2021, Kaldor, Stephen W.; Tyhonas, John; Murphy, Eric A.; Kanouni, Toufike; Arnold, Lee D.; Kania, Robert; Cox, Jason M. published a patent.Safety of 5-Bromo-4-chloro-2-fluoroaniline The title of the patent was Pyrazolecarboxamides as inhibitors of fibroblast growth factor receptor kinases and their preparation. And the patent contained the following:

Provided herein are heteroaryl compounds as inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases. Compounds of formula I wherein Z is (un)substituted alkenoyl, (un)substituted alkynoyl, (un)substituted cyanoacetyl, etc.; R is H, (un)substituted C1-6 alkyl, (un)substituted C3-7 carbocyclyl, (un)substituted C3-7 heterocyclyl, etc.; R4 is (un)substituted 9- to 10-membered heteroaryl; R6 is (un)substituted alkyl (un)substituted carbocyclylalkyl and (un)substituted heterocyclylalkyl; and pharmaceutically acceptable salts and solvates thereof, are claimed. Example compound II was prepared by coupling of 3-bromo-1-[(3S,5R)-5-(methoxymethyl)-1-(prop-2-enoyl)pyrrolidin-3-yl]-5-(methylamino)pyrazole-4-carboxamide and 5-ethynyl-2-methylbenzimidazole. The invention compounds were evaluated for their FGFR2 kinase inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of ≤ 0.10μM. The experimental process involved the reaction of 5-Bromo-4-chloro-2-fluoroaniline(cas: 111010-07-2).Safety of 5-Bromo-4-chloro-2-fluoroaniline

The Article related to pyrazolecarboxamide preparation fgfr2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Safety of 5-Bromo-4-chloro-2-fluoroaniline

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

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