Category: bromides-buliding-blocks

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

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

Wang, Lin; Fang, Zhijie published an article in 2020, the title of the article was Study on the synthesis and biological activities of N-alkylated deoxynojirimycin derivatives with a terminal tertiary amine.Electric Literature of 574-98-1 And the article contains the following content:

A series of N-alkylated deoxynojirimycin (DNJ) derivatives I (n = 1, 3; R = R1 = Me; RR1 = -(CH2)4-, -(CH2)5-, -(CH2)2O(CH2)2-) connected to a terminal tertiary amine at the alkyl chains of various lengths was prepared These novel synthetic compounds I were assessed for preliminary glucosidase inhibition and anticancer activities in vitro. Potent and selective inhibition was observed among them. Compound I (n = 1; RR1 = -(CH2)2O(CH2)2-) II (IC50 = 0.052μM) showed improved and selective inhibitory activity against β-glucosidase compared to DNJ (IC50 = 0.65μM). In addition, anal. of the kinetics of enzyme inhibition by using Lineweaver-Burk plots indicated that II inhibited β-glucosidase in a competitive manner, suggesting that II was expected to bind to the active site of β-glucosidase. Compounds I [n = 3; RR1 = -(CH2)4-, -(CH2)5-] were found to be moderate and selective inhibitors of α-glucosidase. Nevertheless, none of compounds inhibited the growth of B16F10 melanoma cells. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Electric Literature of 574-98-1

The Article related to tertiary amine alkyl deoxynojirimycin preparation glucosidase inhibition antitumor activity, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.Electric Literature of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 22, 2022, Zhou, Jiajun; Li, Mao; Wu, Jiadong; Zhang, Chongyin; He, Zidong; Xiao, Yan; Tong, Gangsheng; Zhu, Xinyuan published an article.SDS of cas: 574-98-1 The title of the article was One-pot synthesis of hydroxyl terminated hyperbranched semi-aromatic Poly(ester-imide)s. And the article contained the following:

A new kind of hyperbranched semi-aromatic poly(ester-imide)s with hydroxyl terminated groups has been prepared from com. available 1,2,4-benzenetricarboxylic anhydride (TMA) as the AA’-type aromatic monomer and 3-amino-1,2-propanediol (3APPD), 2-amino-1,3-propanediol (2APPD), N,N-bis(2-hydroxyethyl)ethylenediamine (BHED) as CB2-type aliphatic monomers via a simple one-pot melting polymerization method. The effects of synthesis conditions on the structures and properties of the products were investigated in detail. The combination of FTIR, 1H NMR, 2D NMR, MALDI-FTICR-MS and model reactions have been used to characterize the structures of the obtained polymers. As assessed using thermal measurements, the obtained hyperbranched semi-aromatic poly(ester-imide)s possess low glass transition temperature (≤120°C) and high thermostability with an onset decomposition temperature ranging from 355 to 420°C in nitrogen. The products possess abundant terminal hydroxyl functional groups. Hydroxyl values vary between 198 and 248 mg KOH/g depending on the particular precursors used to generate the polymers. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).SDS of cas: 574-98-1

The Article related to pot hydroxyl terminated hyperbranched semiarom polyesterimide, Plastics Manufacture and Processing: Preparation Of Resins and other aspects.SDS of cas: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 30, 2020, Ruan, Qing; Zhang, Xuran; Zhang, Junbo published an article.COA of Formula: C10H8BrNO2 The title of the article was Radiosynthesis and evaluation of novel [99mTc(I)]+ and [99mTc(I)(CO)3]+ complexes with a 4-nitroimidazole isocyanide for imaging tumor hypoxia. And the article contained the following:

[99mTc(I)]+ and [99mTc(I)(CO)3]+ complexes with isocyanide exhibit high stability, which makes them suitable platforms to develop novel 99mTc radiopharmaceuticals. To develop novel 99mTc radiotracers for imaging hypoxia, a novel L ligand (4-nitroimidazole isocyanide derivative) was synthesized and labeled using [99mTc(I)]+ core and [99mTc(I)(CO)3]+ core to produce [99mTc(L)6]+ and [99mTc(CO)3(L)3]+ with high yields. To verify the structure of the 99mTc complexes, corresponding rhenium analogs were synthesized and characterized. Both of the 99mTc complexes were stable and hydrophilic. in vitro cellular uptake results showed they could exhibit good hypoxic selectivity. The evaluation of biodistribution in mice bearing S180 tumors indicated both of them could accumulate in tumor. Between them, [99mTc(L)6]+ exhibited higher tumor uptake and tumor/non-target ratio than [99mTc(CO)3(L)3]+. Further, single photon emission computed tomog. (SPECT) imaging studies of [99mTc(L)6]+ indicated an obvious accumulation in tumor and the value of the region-of-interest (ROI) ratio of the uptake for the tumor site to the corresponding non-tumor region was 5.64 ± 0.52. The above results suggested [99mTc(L)6]+ would be a potential tracer for imaging tumor hypoxia. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).COA of Formula: C10H8BrNO2

The Article related to technetium rhenium nitroimidazole isocyanide imaging complex preparation, imaging tumor hypoxia technetium rhenium nitroimidazole isocyanide complex, Inorganic Chemicals and Reactions: Coordination Compounds and other aspects.COA of Formula: C10H8BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 1, 2020, Rezaeivala, Majid; Ahmadi, Musa; Captain, Burjor; Bayat, Mehdi; Saeidirad, Mahdi; Sahin-Bolukbasi, Serap; Yildiz, Batuhan; Gable, Robert William published an article.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Some new morpholine-based Schiff-base complexes; Synthesis, characterization, anticancer activities and theoretical studies. And the article contained the following:

A new morpholine-based ligand (2) has been prepared from condensation of a branched amine containing morpholine, N1-(3-morpholinopropyl)-N1-((pyridine-2-yl)methyl)ethane-1,2-diamine (1), and salicylaldehyde. Metal complexes were synthesized by reaction of the ligand and metal salts in ethanol and the resulting products were characterized by elemental analyses, ESI-MS, 1H and 13C NMR spectra, IR, and UV-Vis spectroscopy. The structure of two complexes including [ZnL](ClO4) (3) and [NiHL](ClO4)·H2O (6a) have been determined by single crystal X-ray structural anal., showing that the metal atoms are in a distorted trigonal bipyramidal (Zn) and a square planar (Ni) environment, resp. Compounds were assayed for their anticancer activities against a panel of human tumor cell lines, including breast cancer cells (MCF-7, MDA-MB-231), prostate cancer cells (PC-3) and human normal lung fibroblast cells (WI-38). Compounds 1, 2, 7, 9 and 10 demonstrated lower activity against MCF-7, MDA-MB-231 and PC-3 cell lines (IC50s > 100μM) compared to other compounds It has been shown that complexes 3, 4, 5, 6, and 8 possess different anticancer potentials against MCF-7, MDA-MB-231 and PC-3. More importantly, it was observed that compounds 3, 5 and 6 demonstrate a lower activity against WI-38 normal cell line than they do against cancer cell lines. Our results indicated that compound 8 has the highest anticancer activity on cancer cell lines, and the reason for that can be attributed to the presence of a silver atom in the complex. These results clearly showed that the anticancer activities of these compounds depend on the type of metal in the complex as well as the tested cancer cell line. Furthermore, the geometries of the [ML]n+ (M = Zn2+, Cd2+, Mn2+, Cu2+, Ni2+, Ag+, Fe3+ and Co2+, n = 0, 1, 2) complexes have been optimized at the BP86/def2-SVP level of theory. The nature of M → L bonds in [ML]n+ complexes have been studied with the help of NBO anal. 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 transition metal morpholine schiff base complex preparation anticancer activity, crystal structure transition metal morpholine schiff base complex, Inorganic Chemicals and Reactions: Coordination Compounds and other aspects.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary