Tag: 200-300

On June 2, 2022, Watanabe, Hideyuki; Kamikubo, Takashi; Kamikawa, Akio; Washio, Takuya; Seki, Yohei; Okuyama, Keiichiro; Ikeda, Osamu; Tomiyama, Hiroshi; Iwai, Yoshinori; Nakamura, Akihiko; Miyasaka, Kozo published a patent.Electric Literature of 1805937-67-0 The title of the patent was Preparation of heteroaryl carboxamide compounds as DGKζ (DGKzeta) inhibitors and anticancer agents. And the patent contained the following:

Heteroaryl carboxamide compounds including N-phenyl-1H-pyrazole-3-carboxamides, N-phenyl-2-oxo-1,2-dihydropyridine-3-carboxamides, and N-phenyloxazole-4-carboxamides represented by formula I [A = Q1, Q2, Q3, or Q4; B = Q5, Q6, Q7, or Q8; when R1 a = halo-C1-6 alkyl, B = Q5; R1a = pyridazinyl or halo-C1-6 alkyl; R1b = H or C1-6 alkyl; R2 = C3-5 cycloalkyl, C1-6 alkyloxy, halo-C1-6 alkyl, halo, or Ph; R3 = each (un)substituted Ph, C3-8 cycloalkyl, or pyridyl, or 5- or 6-membered partially unsaturated heterocyclyl containing 1-4 heteroatoms selected from O, S, and N atoms; R4 = H or F; R6 = -L2-(CH2)2NRaRb, or piperidinyl; L1 = a singe bond, O, or NH; L2 = a single bond, O, or CH2; X = CH2 or NMe; Y = CH or N; Ra = H or Me; Rb = H, Me, Et, cyclopropyl, or (CH2)2OMe; m = 1, 2, or 3] or salts thereof are prepared The compounds I or salts thereof have a DGKζ (DGKzeta) inhibiting activity and are useful as active ingredients for pharmaceutical compositions for treating cancer associated with the activation of an immunocyte or cancer having resistance to an anti-PD-1 antibody/anti-PD-L1 antibody therapy. Thus, [[(2R)-4-[6-amino-3-(2-fluorophenoxy)-2-(trifluoromethyl)phenyl]-1-methylpiperazin-2-yl]methyl](methyl)carbamic acid tert-Bu ester was condensed with 1-(pyridazin-4-yl)-1H-pyrazole-3-carboxylic acid using HATU in the presence of diisopropylethylamine in DMF at 50° for 12 h to give [[(2R)-4-[3-(2-fluorophenoxy)-6-[[[1-(pyridazin-4-yl)-1H-pyrazol-3-yl]carbonyl]amino]-2-(trifluoromethyl)phenyl]-1-methylpiperazin-2-yl]methyl](methyl)carbamic acid tert-Bu ester which was treated with CF3CO2H in CH2Cl2 at room temperature for 4 h followed by purification using silica gel chromatog. (CHCl3/MeOH/aqueous ammonia solution) to give N-[4-(2-fluorophenoxy)-2-[(3S)-4-methyl-3-[(methylamino)methyl]piperazin-1-yl]-3-(trifluoromethyl)phenyl]-1-(pyridazin-4-yl)-1H-pyrazole-3-carboxamide (II). II, II monobutanedioate, and compound (III) showed IC50 of 10, 3.2, 0.42 nM, resp., against human recombinant DGKζ (DGKzeta). The experimental process involved the reaction of 2-Bromo-4-fluoro-1-nitro-3-(trifluoromethyl)benzene(cas: 1805937-67-0).Electric Literature of 1805937-67-0

The Article related to antibody immunotherapy resistant cancer treatment, heteroaryl carboxamide preparation dgkzeta inhibitor anticancer, phenylpyrazolecarboxamide phenyloxodihydropyridinecarboxamide phenyloxazolecarboxamide preparation dgkzeta inhibitor anticancer and other aspects.Electric Literature of 1805937-67-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 31, 2014, Ko, Soo Sung; Batt, Douglas A.; Bertrand, Myra Beaudoin; Delucca, George V.; Langevine, Charles M.; Liu, Qingjie; Srivastava, Anurag S.; Watterson, Scott Hunter published a patent.Recommanded Product: 1-Bromo-3-isocyanato-2-methyl-benzene The title of the patent was Preparation of 4-phenylcarbazole-1-carboxamide compounds useful as Bruton’s tyrosine kinase (Btk) inhibitors. And the patent contained the following:

There are disclosed carbazolecarboxamide compounds of formula [I; Q = Q1, Q2, Q3, or Q4; R1 = C(CH3)2OH, NHC(O)C(CH3)3, N(CH3)2, or CH2Rd; R2 = Cl or CH3; R3 = H, F, or CH3; Ra = H or CH3; Rb = H, F, Cl, or OCH3; Rc = H or F; Rd = OH, OCH3, NHC(O)CH3, or pyrrolidin-1-yl] or salts thereof. These compounds are inhibitors of kinases, in particular Bruton’s tyrosine kinase (Btk) and are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and chronic inflammatory diseases. Thus, 4-bromo-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide was coupled with 5-chloro-2-[2-methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-1H-pyrido[1,2-c]pyrimidine-1,3(2H)-dione in the presence of Pd2(dppf).CH2Cl2adduct and Cs2CO3 in THF under argon at 45° for 3.5 h to give 39% 4-[3-(5-chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrimidin-2(3H)-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide as a mixture of 4 diastereomers which was separated by chiral super-critical fluid chromatog. to give 4-[3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrimidin-2(3H)-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide (II) and 4-[3-(S)-(5-chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrimidin-2(3H)-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide (III). III showed IC50 of 0.41 and 1,000 nM against human recombinant Bruton’s tyrosine kinase (Btk) and Jak2 tyrosine kinase, resp. The experimental process involved the reaction of 1-Bromo-3-isocyanato-2-methyl-benzene(cas: 1261475-16-4).Recommanded Product: 1-Bromo-3-isocyanato-2-methyl-benzene

The Article related to carbazolecarboxamide preparation bruton tyrosine kinase btk kinase inhibitor, phenylcarbazolecarboxamide preparation kinase inhibitor, autoimmune disease chronic inflammatory disease treatment prevention phenylcarbazolecarboxamide preparation and other aspects.Recommanded Product: 1-Bromo-3-isocyanato-2-methyl-benzene

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On August 5, 2020, Sidhu, Jagpreet Singh; Raj, Pushap; Pandiyan, Thangarasu; Singh, Narinder published an article.Formula: C10H8BrNO2 The title of the article was Synthesis of Nickel(II) Complexes of Novel Naphthalimide Based Heterodipodal Schiff Base Ligands, Structure, Characterization and Application for Degradation of Pesticides. And the article contained the following:

To degrade the highly toxic pesticide into less harmful components, authors have synthesized four nickel complexes of naphthalimide based organic ligands. These complexes catalyze the hydrolysis of phosphorothioate bonds of organophosphates in an aqueous medium. The metal complexes {[Ni(L1)2]-[Ni(L4)2]} were synthesized by the electrochem. method and characterized using single-crystal x-ray crystallog. and mass spectrometry. Anal. techniques revealed that complexes are mononuclear and possess octahedral geometry. The rate of degradation of chlorpyriphos and parathion Me was evaluated using 31P NMR and LC-MS chromatogram. The byproduct of chlorpyriphos upon catalytic degradation with complex was confirmed from mass spectrometry. It was found that chlorpyriphos degrade into 3,5,6-trichloropyridin-2-ol after 50 min of incubation with catalyst. However, parathion Me took only 20 min to hydrolyze into its byproduct. Moreover, the inhibition assay of acetylcholinesterase was performed for pesticides in the presence of metal complex and the interesting outcome was recorded. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Formula: C10H8BrNO2

The Article related to nickel naphthalimide heterodipodal schiff base preparation degrade pesticide, crystal mol structure naphthalimide heterodipodal schiff base, phosphorothioate organophosphate hydrolysis catalyst naphthalimide heterodipodal schiff base nickel and other aspects.Formula: C10H8BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On March 1, 2022, Meng, Depei; Lyu, Yichong; Ni, Chuanfa; Zhou, Min; Li, Yang; Hu, Jinbo published an article.Electric Literature of 2567-29-5 The title of the article was S-(Trifluoromethyl)Benzothioate (TFBT): A KF-Based Reagent for Nucleophilic Trifluoromethylthiolation. And the article contained the following:

S-(Trifluoromethyl)benzothioate (TFBT) was developed as an inexpensive, bench-stable and user-friendly trifluoromethylthiolation reagent which was easily synthesized by using KF as the only fluorine source. By using TFBT, trifluoromethylthiolates with various counterions was readily obtained. The synthetic application of TFBT was demonstrated by trifluoromethylthiolation-halogenation of arynes, bis(trifluoromethylthiolation)-halogenation of 1,2-benzdiynes, nucleophilic substitution of alkyl halides, deoxytrifluoromethylthiolation of alcs., and cross-coupling with aryl and vinyl boronic acids. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Electric Literature of 2567-29-5

The Article related to trifluoromethyl benzothioate preparation aryne halogenation trifluoromethylthiolation, halo trifluoromethylthio arene preparation, s-(trifluoromethyl)benzothioate, aryne, multifunctionalization, potassium fluoride, trifluoromethylthiolation and other aspects.Electric Literature of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Yang, Wu; Li, Yingzi; Zhu, Jiefeng; Liu, Wentan; Ke, Jie; He, Chuan published an article in 2020, the title of the article was Lewis acid-assisted Ir(III) reductive elimination enables construction of seven-membered-ring sulfoxides.COA of Formula: C13H11Br And the article contains the following content:

Iridium has played an important role in the evolution of C-H activation chem. over the last half century owing to its high reactivity towards stoichiometric C-H bond cleavage; however, the use of Ir(III) complexes in catalytic C-H functionalization/C-C bond formation appears to have fallen off significantly. The main problem lies in the reductive elimination step, as iridium has a tendency to form stable and catalytically inactive Ir(III) species. Herein, with a rationally designed Lewis acid assisted oxidatively induced strategy, the sluggish Ir(III) reductive elimination is successfully facilitated, enabling the facile C-C bond formation. The X-ray crystal structure of a silver salt adduct of iridacycle and DFT calculations demonstrate that the sulfoxide group acts as a key bridge connecting the Ir(III) metal center with the silver Lewis acid, which facilitates the reductive elimination of the Ir(III) metallacycle. Further identification of oxidants was carried out by performing stoichiometric reactions, which enables the development of catalytic construction of various highly functionalized seven-membered-ring sulfoxides e.g., 5,7-dihydrodibenzo[c,e]thiepine 6-oxide, that are of great interest in medicinal chem. and materials science. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).COA of Formula: C13H11Br

The Article related to dihydrodibenzothiepine oxide preparation chemoselective regioselective density functional theory, aralkyl sulfoxide oxidative reductive elimination lewis acid iridium catalyst and other aspects.COA of Formula: C13H11Br

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On March 15, 2022, Grant, Thomas M.; Rennison, David; Cervin, Gunnar; Pavia, Henrik; Hellio, Claire; Foulon, Valentin; Brimble, Margaret A.; Cahill, Patrick; Svenson, Johan published an article.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Towards eco-friendly marine antifouling biocides – Nature inspired tetrasubstituted 2,5-diketopiperazines. And the article contained the following:

Marine biofouling plagues all maritime industries at vast economic and environmental cost. Previous and most current methods to control biofouling have employed highly persistent toxins and heavy metals, including tin, copper, and zinc. These toxic methods are resulting in unacceptable environmental harm and are coming under immense regulatory pressure. Eco-friendly alternatives are urgently required to effectively mitigate the neg. consequence of biofouling without causing collateral harm. Amphiphilic micropeptides have recently been shown to exhibit excellent broad-spectrum antifouling activity, with a non-toxic mode of action and innate biodegradability. The present work focused on incorporating the pharmacophore derived from amphiphilic micropeptides into a 2,5-diketopiperazine (DKP) scaffold. This privileged structure is present in a vast number of natural products, including marine natural product antifoulants, and provides advantages of synthetic accessibility and adaptability. A novel route to sym. tetrasubstituted DKPs was developed and a library of amphiphilic 2,5-DKPs were subsequently synthesized. These biodegradable compounds were demonstrated to be potent marine antifoulants displaying broad-spectrum activity in the low micromolar range against a range of common marine fouling organisms. The outcome of planned coating and field trials will dictate the future development of the lead compounds 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 ciona undaria diketopiperazine marine antifouling biocides pharmacophore amphiphilic micropeptides, antifouling, broad-spectrum, diketopiperazine, marine, non-toxic, synthesis and other aspects.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Halik, Pawel K.; Lipinski, Piotr F. J.; Matalinska, Joanna; Kozminski, Przemyslaw; Misicka, Aleksandra; Gniazdowska, Ewa published an article in 2020, the title of the article was Radiochemical synthesis and evaluation of novel radioconjugates of neurokinin 1 receptor antagonist aprepitant dedicated for NK1R-positive tumors.Recommanded Product: 574-98-1 And the article contains the following content:

Aprepitant, a lipophilic and small mol. representative of neurokinin 1 receptor antagonists, is known for its anti-proliferative activity on numerous cancer cell lines that are sensitive to Substance P mitogen action. In the presented research, we developed two novel structural modifications of aprepitant to create aprepitant conjugates with different radionuclide chelators. All of them were radiolabeled with 68Ga and 177Lu radionuclides and evaluated in terms of their lipophilicity and stability in human serum. Furthermore, fully stable conjugates were examined in mol. modeling with a human neurokinin 1 receptor structure and in a competitive radioligand binding assay using rat brain homogenates in comparison to the aprepitant mol. This initial research is in the conceptual stage to give potential theranostic-like radiopharmaceutical pairs for the imaging and therapy of neurokinin 1 receptor-overexpressing cancers. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 574-98-1

The Article related to aprepitant radiopharmaceutical neurokinin receptor antagonist radionuclide chelator, aprepitant, neurokinin 1 receptor antagonist, radionuclide chelators, radiopharmaceuticals and other aspects.Recommanded Product: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 1, 2021, Ibanez-Escribano, Alexandra; Reviriego, Felipe; Vela, Nerea; Fonseca-Berzal, Cristina; Nogal-Ruiz, Juan Jose; Aran, Vicente J.; Escario, Jose Antonio; Gomez-Barrio, Alicia published an article.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Promising hit compounds against resistant trichomoniasis: Synthesis and antiparasitic activity of 3-(ω-aminoalkoxy)-1-benzyl-5-nitroindazoles. And the article contained the following:

A series of 11 3-(ω-aminoalkoxy)-1-benzyl-5-nitroindazoles has been prepared starting from 1-benzyl-5-nitroindazol-3-ol, and evaluated against sensitive and resistant isolates of the sexually transmitted protozoan Trichomonas vaginalis. A variety of nitroindazoles demonstrate trichomonacidal profiles with IC50 < 20μM against the metronidazole-sensitive isolate. Moreover, all these compounds submitted to cytotoxicity assays against mammalian cells exhibited low non-specific cytotoxic effects, except two compounds I and II which displayed moderate cytotoxicity (CC50 = 74.7 and 59.1μM, resp.). Those compounds with trichomonacidal effect were also evaluated against a metronidazole-resistant culture. Special mention deserve compounds III and IV, which displayed better IC50 values (1.3 and 0.5μM resp.) than that of the reference drug (IC50 MTZ = 3.0μM). The high activity of these compounds against the resistant isolate reinforces the absence of cross-resistance with the reference drug. The remarkable trichomonacidal results against resistant T. vaginalis isolates suggest the interest of 3-(ω-aminoalkoxy)-1-benzyl-5-nitroindazoles to be considered as good prototypes to continue in the development of new drugs with enhanced trichomonacidal activity, aiming to increase the non-existent drugs to face clin. resistance efficiently for those patients in whom therapy with 5-nitroimidazoles is contraindicated. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to aminoalkoxy benzyl nitroindazole preparation antiparasitic resistant trichomoniasis, antiprotozoal agents, indazole, nitrogen heterocycles, resistance, trichomonas vaginalis and other aspects.Quality Control of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Fonseca-Berzal, Cristina; Ibanez-Escribano, Alexandra; Vela, Nerea; Cumella, Jose; Nogal-Ruiz, Juan Jose; Escario, Jose Antonio; Bernardino da Silva, Patricia; Batista, Marcos Meuser; Soeiro, Maria de Nazare C.; Sifontes-Rodriguez, Sergio; Meneses-Marcel, Alfredo; Gomez-Barrio, Alicia; Aran, Vicente J. published an article in 2018, the title of the article was Antichagasic, Leishmanicidal, and Trichomonacidal Activity of 2-Benzyl-5-nitroindazole-Derived Amines.Recommanded Product: 574-98-1 And the article contains the following content:

Three different series of new 5-nitroindazole derivatives-1-(ω-aminoalkyl)-2-benzylindazolin-3-ones (series A; ten compounds), 3-(ω-aminoalkoxy)-2-benzylindazoles (series B; four compounds) and 3-alkylamino-2-benzylindazoles (series C; five compounds)-have been synthesized and evaluated against the protozoan parasites Trypanosoma cruzi, Leishmania amazonensis, and Trichomonas vaginalis: etiol. agents of Chagas disease, cutaneous leishmaniasis, and trichomoniasis, resp. Many indazoles of series A, B, and C were efficient against T. cruzi. Some compounds in series A, after successfully passing the preliminary screening for epimastigotes, exhibited activity values against amastigotes of several T. cruzi strains that were better than or similar to those shown by the reference drug benznidazole and displayed low nonspecific toxicity against mammalian cells. On the other hand, preliminary studies against promastigotes of L. amazonensis showed high leishmanicidal activity for some derivatives of series A and C. With regard to activity against T. vaginalis, some indazoles of series B and C were rather efficient against trophozoites of a metronidazole-sensitive isolate and showed low nonspecific toxicities toward Vero cell cultures. Addnl., some of these compounds displayed similar activity against metronidazole-sensitive and resistant isolates, showing the absence of cross-resistance between these derivatives and the reference drug. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 574-98-1

The Article related to benzyl nitroindazole amine antichagasic leishmanicidal trichomonacidal activity, antiprotozoal agents, leishmaniasis, nitrogen heterocycles, trichomoniasis, trypanosomiasis and other aspects.Recommanded Product: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 26, 2021, Ravula, Thirupathi; Ramamoorthy, Ayyalusamy published an article.Application In Synthesis of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Synthesis, Characterization, and Nanodisc Formation of Non-ionic Polymers. And the article contained the following:

Although lipid nanodiscs are increasingly used in the structural studies of membrane proteins, drug delivery and other applications, the interaction between the nanodisc belt and the protein to be reconstituted is a major limitation. To overcome this limitation and to further broaden the scope of nanodiscs, a family of non-ionic amphiphilic polymers synthesized by hydrophobic functionalization of fructo-oligosaccharides/inulin is reported. We show the stability of lipid nanodiscs formed by these polymers against pH and divalent metal ions, and their magnetic-alignment properties. The reported results also demonstrate that the non-ionic polymers extract membrane proteins with unprecedented efficiency. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Application In Synthesis of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to nanodisc nonionic functionalization fructo oligosaccharide inulin nanodisc, membrane protein inulin functionalized, lipids, nanodiscs, non-ionic polymers, oligosaccharides and other aspects.Application In Synthesis of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary