Tag: 200-300

On September 30, 2018, Lin, Xiao; Ruan, Qing; Lin, Ling; Zhang, Xuran; Duan, Xiaojiang; Teng, Yanguo; Zhang, Junbo published an article.Recommanded Product: 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Biological evaluation and SPECT imaging of tumor hypoxia using a novel technetium-99m labeled tracer with 2-nitroimidazole moiety. And the article contained the following:

To develop novel 99mTc labeled nitroimidazole imaging agents for imaging tumor hypoxia, 99mTc labeled ethylene diamine tetraacetic acid derivative of 4-nitroimidazole was reported by us earlier, which showed disadvantage of an unsatisfactory tumor-to-blood ratio. Therefore, 2-nitroimidazole was adopted as a pharmacophore to synthesize EDTA-2-EtNHNM, which was radiolabeled with 99mTc in high yield to achieve 99mTc-EDTA-2-EtNHNM. 99mTc-EDTA-2-EtNHNM was hydrophilic and exhibited good in vitro stability. Cellular experiment demonstrated its hypoxic selectivity while biodistribution results showed improved tumor-to-blood and tumor-to-muscle ratios. SPECT imaging studies of 99mTc-EDTA-2-EtNHNM indicated obvious accumulation in tumor, suggesting its potential to be a radiotracer for imaging tumor hypoxia. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to spect imaging tumor hypoxia technetium 99m nitroimidazole, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Recommanded Product: 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 17, 2014, Li, Yun-Long; Burns, David M.; Feng, Hao; Xue, Chu-Biao; Wang, Anlai; Pan, Jun published a patent.HPLC of Formula: 1196157-51-3 The title of the patent was Preparation of bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors for treating proliferative and immune disorders. And the patent contained the following:

The present disclosure describes bicyclic aromatic carboxamide derivatives of formula I (wherein Cy is (un)substituted C3-7 cycloalkyl or (un)substituted 4-10 membered heterocycloalkyl; A1 is N or (un)substituted CH; R2 is H, halogen, C1-6 alkyl, etc.; or A1 and R2 together form part of a ring; R3 is H, halogen or NH2; R4 is H or halogen; and A5-A8 are independently N or (un)substituted CH, with provisos), as well as their compositions and methods of use as Pim kinase inhibitors for treating cancer and other diseases. Synthetic procedures for preparing I are exemplified. Example compound II was prepared in a 6-step synthesis that involved reaction of intermediate III with benzyl [(3S)-1-(3-aminopyridin-4-yl)piperidin-3-yl]carbamate followed by deprotection of the intermediate formed to give II. In Pim kinase inhibitory assays in vitro, II had IC50 values of ≤100 nM for Pim1 and Pim3 and an IC50 value between 100 nM and 1000 nM for Pim2 kinase. The experimental process involved the reaction of 2-Amino-6-bromonicotinic acid(cas: 1196157-51-3).HPLC of Formula: 1196157-51-3

The Article related to preparation bicyclic aromatic carboxamide compound pim kinase inhibitor therapy, proliferative immune disorder treatment bicyclic aromatic carboxamide compound, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 1196157-51-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 29, 2001, Astles, Peter C.; Eastwood, Paul R.; Houille, Olivier; Levell, Julian; Pauls, Heinz; Czekaj, Mark; Liang, Guyan; Gong, Yong; Pribish, James; Neuenschwander, Kent published a patent.Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene The title of the patent was Preparation of (hetero)arylacyl-piperidinyl-benzylamines for use as tryptase inhibitors. And the patent contained the following:

Title compounds I [Ar = (hetero)aryl, where the two groups on the Ar ring are β to each other; R1-2 = H, alkyl; R3 = (un)substituted(hetero)aryl, arylalkenyl, cycloalkenyl, cycloalkyl, etc.; R4 = H, acyl, alkoxy, alkyloxycarbonyl, carboxy, CN, halo, etc.; n = 0 – 4] were prepared Over 300 synthetic examples were disclosed. For instance, 3-bromobenzylbromide was converted in two steps to boronate II. II was coupled to the triflate ester derivative of the enol of 4-oxo-N-benzyloxycarbonylpiperidine (DMF, K2CO3, PdCl2(dppf)•CH2Cl2, 80°C, 18 h) to give the corresponding bicyclic intermediate. This intermediate was deprotected and reduced to the piperidine (EtOH, 10% Pd-C/H2, room temperature, 5 h) and coupled to 5-phenethylthiophene-2-carboxylic acid (DMF, HAPyU, iPr2NEt, room temperature, 18 h) to give III. III had Ki = 50 nM for tryptase. I are useful in the treatment of e.g., asthma and inflammatory diseases. The experimental process involved the reaction of 2-Bromo-4-(bromomethyl)-1-methylbenzene(cas: 259231-26-0).Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene

The Article related to piperidinylbenzylamine tryptase inhibitor preparation, pyridine quinoline thiophene furan indole piperidine tryptase inhibitor preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 19, 2022, Grollier, Kevin; Ghiazza, Clement; Tlili, Anis; Billard, Thierry; Medebielle, Maurice; Vantourout, Julien C. published an article.Computed Properties of 2567-29-5 The title of the article was Electrochemical Trifluoromethylselenolation of Activated Alkyl Halides. And the article contained the following:

A practical electrochem. method for the generation of CF3Se- anion from a shelf-stable reagent (TsSeCF3) is reported allowing the metal-free trifluoromethylselenolation of activated alkyl halides RCH2X (X = Br, Cl; R = 4-F-Ph, pyridin-2-yl, 5-nitrofuran-2-yl, undecyl, etc.). Trifluoromethylselenolated compounds RCH2SeCF3 have been obtained in modest to excellent yields under the optimized reaction conditions. Finally, cyclic voltammetric and 19F NMR studies are presented and allowed to gain insight into the reaction mechanism. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Computed Properties of 2567-29-5

The Article related to trifluoromethylselenolate preparation electrochem, trifluoromethyltolueneselenosulfonate alkyl halide trifluoromethylselenolation, Aliphatic Compounds: (This Subsection Discontinued) and other aspects.Computed Properties of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 29, 2021, Kang, Kai; Loud, Nathan L.; DiBenedetto, Tarah A.; Weix, Daniel J. published an article.SDS of cas: 574-98-1 The title of the article was A General, Multimetallic Cross-Ullmann Biheteroaryl Synthesis from Heteroaryl Halides and Heteroaryl Triflates. And the article contained the following:

A new, general approach to biheteroaryls: the Ni- and Pd-catalyzed multimetallic cross-Ullmann coupling of heteroaryl halides with triflates. An array of 5-membered, 6-membered and fused heteroaryl bromides and chlorides, as well as aryl triflates derived from heterocyclic phenols proved to be viable substrates in this reaction (62 examples, 63 ± 17% average yield). The generality of this approach to biheteroaryls were further demonstrated in 96-well plate format at 10μmol scale. An array of 96 possible products provided >90% hit rate under a single set of conditions. Further, low-yielding combinations was rapidly optimized with a single “Toolbox Plate” of ligands, additives and reductants. 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 pyridyl trifluoromethanesulfonate heteroaryl halide nickel palladium catalyst ullmann coupling, heteroaryl pyridine preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.SDS of cas: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 15, 2021, Chen, Xin; Yang, Xi; Mao, Fei; Wei, Jinlian; Xu, Yixiang; Li, Baoli; Zhu, Jin; Ni, Shuaishuai; Jia, Lijun; Li, Jian published an article.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Development of novel benzimidazole-derived neddylation inhibitors for suppressing tumor growth invitro and invivo. And the article contained the following:

In this study, I [R = H, aminopropane(CO), aminocyclopropane(CO),..etc]. were designed and synthesized based on lead compound CDC to improve the neddylation inhibition and anticancer efficacy. Optimal benzimidazole-derived I [R = (2,4-dichlorophenyl)-1-ethylamino(CO)] displayed superior neddylation inhibition in enzyme assay compared to CDC (IC50 = 5.51μM vs 16.43μM), along with promising target inhibitory activity and killing selectivity in cancer cell. The results of cellular mechanism research combined with tumor growth suppression in human lung cancer cell A549 in vivo, accompanied with docking model, revealed that I [R = (2,4-dichlorophenyl)-1-ethylamino(CO)] had the potential to be developed as a promising neddylation inhibitor for anticancer therapy. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Quality Control of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to benzimidazolyl methylbiphenylyl tetrazole preparation antitumor agent sar enzyme inhibitor, anticancer, benzimidazole-derived inhibitor, neddylation, cullin1-nedd8, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On August 5, 2004, Poupart, Marc-Andre; Beaulieu, Pierre Louis; Rancourt, Jean published a patent.Application In Synthesis of Methyl 5-bromo-2-methoxy-4-methylbenzoate The title of the patent was A preparation of heterocyclic compounds, useful as inhibitors of RNA dependent RNA polymerases, such as hepatitis C virus polymerase. And the patent contained the following:

The invention relates to a preparation of heterocyclic compounds of formula I [wherein: R1 is (cyclo)alkyl, cycloalkenyl, 4 to 7-membered heterocyclic ring, etc.; R2 is halogen or (un)substituted (hetero)aryl; B is N and A is :CH-, or :N-, etc.; B is :C- and A is O, S, or NH, etc.; M1 and M4 are independently selected from CR3; M2 and M3, when not linked to -C(:Y)Z, is CR3; R3 is H, halogen, CN, or azido, etc.], useful as inhibitors of RNA dependent RNA polymerases, particularly those viral polymerases within Flaviviridae family, more particularly to hepatitis C virus (HCV) polymerase. For instance, NS5B RNA dependent RNA polymerase inhibition of pyridinylindole derivative II was determined (compound 101, table 1; IC50 < 1μM). The experimental process involved the reaction of Methyl 5-bromo-2-methoxy-4-methylbenzoate(cas: 39503-58-7).Application In Synthesis of Methyl 5-bromo-2-methoxy-4-methylbenzoate

The Article related to heterocycle preparation hepatitis c virus hcv rna polymerase inhibitor, flaviviridae hepatitis c virus polymerase inhibitor heterocycle preparation, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Application In Synthesis of Methyl 5-bromo-2-methoxy-4-methylbenzoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 30, 2022, Liang, Xiao; Li, Xue; Zhao, Zhiyuan; Nie, Yiming; Yao, Zefu; Ren, Wandi; Yang, Xinying; Hou, Xuben; Fang, Hao published an article.Category: bromides-buliding-blocks The title of the article was Design, synthesis and biological evaluation of hydantoin derivatives as Mcl-1 selective inhibitors. And the article contained the following:

Herein, authors designed and synthesized a series of hydantoin derivatives I (R1 = H, Ph, OCH2Ph, etc.; R2 = Me, Bn, CH2-Ph-Ph, etc.; R3 = H, 3-NO2-4-Cl) as novel myeloid cell leukemia-1 (Mcl-1) inhibitors based on authors’ previously developed lead compound Among them, compound I (R1 = -OCH2-3,4-di-Cl-Ph; R2 = -CH2-Ph-OCH2-4-Cl-Ph; R3 = 3-NO2-4-Cl) and I (R1 = O(CH2)2-O-3,5-diMe-4-Cl-Ph; R2 = -CH2-Ph-OCH2-4-Cl-Ph; R3 = 3-NO2-4-Cl) exhibited good binding affinities against Mcl-1 with Ki values of 0.49μM and 0.33μM resp. Especially, compound I (R1 = -OCH2-3,4-di-Cl-Ph; R2 = -CH2-Ph-OCH2-4-Cl-Ph; R3 = 3-NO2-4-Cl) exhibited good selectivity over Bcl-xL, whereas compound I (R1 = O(CH2)2-O-3,5-diMe-4-Cl-Ph; R2 = -CH2-Ph-OCH2-4-Cl-Ph; R3 = 3-NO2-4-Cl) possessed good selectivity over both Bcl-2 and Bcl-xL. Furthermore, authors also investigated the effects of these new Mcl-1 inhibitors on cell proliferation, apoptosis and mitochondrial membrane potential, as well as the stability in plasma. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Category: bromides-buliding-blocks

The Article related to hydantoin preparation antitumor human mcl1 inhibitor apoptosis, apoptosis, cancer, hydantoin derivatives, mcl-1 inhibitors, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Shao, Rui; Zhao, Haixia; Ding, Shumin; Li, Lianjie; Chen, Chen; Wang, Jian; Shang, Yongjia published an article in 2022, the title of the article was Silver-promoted dearomative [3+4] cycloaddition of anthranils with α-isocyanoacetates: access to benzodiazepines.SDS of cas: 2567-29-5 And the article contains the following content:

The first example of silver-promoted [3+4] cycloaddition of α-isocyanoacetates with anthranils as aromatic Michael accepters, offering access to benzo[d][1,3]diazepinones. Mechanistic studies revealed that an “oxygen migration” rearrangement process was involved in this dearomative cycloaddition reaction. Addnl., benzo[d][1,3]diazepinones were obtained efficiently as well under catalytic conditions. Broad functional groups were well tolerated under mild reaction conditions. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).SDS of cas: 2567-29-5

The Article related to anthranil isocyanoacetate silver promoter dearomative cycloaddition, dihydrobenzodiazepinone carboxylate preparation, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.SDS of cas: 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 31, 2020, Zhang, Xinwei; Zhang, Cunlong; Tang, Lin; Lu, Kuan; Zhao, Huan; Wu, Weibin; Jiang, Yuyang published an article.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Synthesis and biological evaluation of piperidyl benzimidazole carboxamide derivatives as potent PARP-1 inhibitors and antitumor agents. And the article contained the following:

A series of compounds based on a piperidyl benzimidazole carboxamide structure and tested their PARP-1 inhibitory activity, as well as cellular inhibitory activity. Some of them showed great potency as PARP-1 inhibitors and antitumor activity, which were valuable for further research. In addition, the predicted ADME properties and proposed binding mode with PARP-1 of the compounds were obtained via computational simulation. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to alkyl amidobenzimidazolyl piperidine preparation parp inhibition antitumor sar pharmacokinetics, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary