Month: November 2022

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

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 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

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 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 July 21, 2022, Yang, Dun; Zhang, Jing; Zhang, Shenqiu; Allen, Thaddeus; Shi, Qiong; Nimishetti, Naganna; Huang, Jian; Li, Hongmei; Yang, Chenglu published a patent.Related Products of 259231-26-0 The title of the patent was Preparation of fused azepine compounds and their use in the treatment of cancer. And the patent contained the following:

The invention relates to fused azepines of formula I and pharmaceutically acceptable salts thereof; their preparation and use in the treatment of cancer. Compounds of formula I, wherein X is O and S; ring A is (un)substituted Ph, (un)substituted 6-membered heteroaryl; L is a bond, CO, SO2, etc.; each R1 is independently halo, CN, (un)substituted Ph, etc.; each R2 is H, CN, (un)substituted Ph, etc.; each R3 is (un)substituted Ph, (un)substituted heteroaryl, (un)substituted 3- to 7-membered carbocyclyl, etc.; m = 0 – 4; p = 0 – 5; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by condensation of Me 5-hydroxy-2-oxo-2,3-dihydro-1H-benzo[b]azepine-4-carboxylate with (bromomethyl)benzene. The invention compounds were evaluated for their anticancer activities (some data given). The experimental process involved the reaction of 2-Bromo-4-(bromomethyl)-1-methylbenzene(cas: 259231-26-0).Related Products of 259231-26-0

The Article related to fused azepine treatment cancer preparation, Heterocyclic Compounds (One Hetero Atom): Higher-Membered Rings and other aspects.Related Products of 259231-26-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 1, 2020, Kubasov, A. S.; Turishev, E. S.; Golubev, A. V.; Bykov, A. Yu.; Zhizhin, K. Yu.; Kuznetsov, N. T. published an article.Synthetic Route of 574-98-1 The title of the article was The method for synthesis of 2-sulfonium closo-decaborate anions derivatives with exo-polyhedral aminogroups. And the article contained the following:

A method for the preparation of sulfonium derivatives of the closo-decaborate anion with the exo-polyhedral amino groups [B10H9S((CH2)nNH2)2]- (n = 1-3) has been developed. The method is based on the alkylation of the [B10H9SH]2- anion with N-bromoalkyl phthalimides and subsequent removal of the phthalimide protection with hydrazine. We could show that the interaction between the [B10H9SH]2- anion with bromomethyl phthalimide groups allowed us to prepare selectively mono-S-substituted sulfanyl derivatives [B10H9SCH2N(CO)2C6H4]2-. Due to the high stability of the sulfonium derivatives of the closo-decaborate anion, it is possible to obtain perchlorinated analogs of these compounds by chlorination of the salts n-Bu4N[B10H9S((CH2)nN(CO)2C6H4)2] (n = 1-3) with sulfuryl chloride in acetonitrile. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Synthetic Route of 574-98-1

The Article related to crystal structure mol sulfonium decaborate anion polyhedral amino preparation, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Synthetic Route of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 23, 2022, Long, Alan; Liu, Chun Yu; Liu, Chunliang; Zhou, Yasheen; Pulley, Shon R.; Graham, Keith Andrew Newton published a patent.Product Details of 1160653-94-0 The title of the patent was Boron containing pyrazole compounds, compositions comprising them, methods and uses thereof. And the patent contained the following:

The present invention describes novel boron containing pyrazole compounds, e.g. I, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the invention have activity as Janus kinase (JAK) inhibitors and are useful in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described are methods of treating inflammation, auto-immune diseases, cancer, and other conditions that are susceptible to the inhibition of a Janus kinase by administering a compound herein described. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methoxybenzaldehyde(cas: 1160653-94-0).Product Details of 1160653-94-0

The Article related to boron amidopyrazole preparation janus kinase inhibition autoimmune anticancer, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Product Details of 1160653-94-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 29, 2018, Zhu, Bin published a patent.Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene The title of the patent was Microglial cell IL-1β secretion inhibitor, and its preparation method and application in treatment of neuroinflammatory diseases. And the patent contained the following:

The title microglial cell IL-1β secretion inhibitor is (((2,5-dibromocyclopenta-2,4-diene-1,1-diyl)bis(methylene))bis(6-alkyl-3,1-phenylene))diboronic acid, has structural formula shown as formula I in Claim 1, wherein R is C1-C10 alkyl or C3-C8 cycloalkyl. The invention also provides preparation method of above compound from cyclopenta-1,3-diene, 2-bromo-4-(bromomethyl)-1-alkylbenzene, boric acid, and bromine. The invention also provides application of the microglial cell IL-1β secretion inhibitor in preparation of drugs for treatment of neuroinflammatory 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 bromocyclopenta dienediyl diboronic acid preparation neuroinflammatory disease treatment, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 25, 2022, Yang, Xiaoxu; Ge, Shaozhong published an article.Product Details of 2567-29-5 The title of the article was Cobalt-Catalyzed 1,1,3-Triborylation of Terminal Alkynes. And the article contained the following:

The authors have developed a Co-catalyzed regioselective 1,1,3-triborylation reaction of terminal alkynes with pinacolborane (HBpin) with a catalyst generated in situ from readily available and bench-stable Co(acac)2 and xantphos. A variety of terminal alkynes undergo this triborylation reaction, affording the corresponding 1,1,3-triborylalkanes in good yields with high selectivity. The synthetic utility of this catalytic protocol was demonstrated by developing selective stepwise functionalization of 1,1,3-triborylalkane products. The results of mechanistic studies, such as conducting control experiments and D-labeling reactions, monitoring the reaction process, and identifying reaction intermediates, suggest that this 1,1,3-triborylation reaction proceeds through 1,3-diborylation of alken-1-ylboronates formed by Co-catalyzed hydroboration of terminal alkynes. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Product Details of 2567-29-5

The Article related to terminal alkyne preparation cobalt catalyzed triborylation pinacolborane, triborylalkane preparation reactivity, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Product Details of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary