Author: Jessica.F

On February 10, 2022, Chen, Chen published a patent.Related Products of 111010-07-2 The title of the patent was Preparation of cyclic iminopyridimdine compounds and their bicyclic derivatives as kinase inhibitors and uses thereof. And the patent contained the following:

Provided are the title compounds I [G1 = N or CRa; G2 = N or CRb; n = 1 or 2; m = 0-3; Ra and Rb = (independently) H, halo, CN, etc.; each R1 = (independently) halo, (un)substituted alkyl, alkoxy; or two R1 groups with the carbon atom they connect to form (un)substituted 4-7 membered carbocyclic or heterocyclic ring; R2 = H, (un)substituted alkyl, alkoxy, etc.; R3 = H, halo, (un)substituted alkyl, alkoxy; R4 = H, (un)substituted alkyl, heterocyclyl, etc.; and R5 = H, alkyl, or heterocyclyl; or NR4R5 = (un)substituted heterocyclyl or heteroaryl; with the provisos] or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and methods of using such compounds or compositions, such as methods of treating a proliferation disorder, such as a cancer or a tumor, or in some embodiments disease or disorders related to the dysregulation of kinase such as, but not limited to kinases such as MAPK, PDGFR, Src, PAKs, c-Kit, EphA2, EphB4, FGFR, Axl, and c-Met. E.g., a multi-step synthesis of II, starting from 4-amino-2-(methylthio)pyrimidine-5-carboxaldehyde and Me 2-(2,4-dichlorophenyl)acetate, was described. The effect of the exemplified compounds I on the activity of various kinases were assessed (data given for representative compounds I). The experimental process involved the reaction of 5-Bromo-4-chloro-2-fluoroaniline(cas: 111010-07-2).Related Products of 111010-07-2

The Article related to cyclic iminopyrimidine bicyclic derivative preparation kinase inhibitor antitumor, mapk pdgfr src pak kinase inhibitor imidazopyridopyrimidinamine pyridodipyrimidinamine preparation, ckit epha2 ephb4 kinase inhibitor imidazopyridopyrimidinamine pyridodipyrimidinamine preparation antitumor and other aspects.Related Products of 111010-07-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 1, 2018, Erokhina, Svetlana A.; Stogniy, Marina Yu.; Suponitsky, Kyrill Yu.; Kosenko, Irina D.; Sivaev, Igor B.; Bregadze, Vladimir I. published an article.COA of Formula: C10H8BrNO2 The title of the article was Synthesis of new nido-carborane based carboxylic acids and amines. And the article contained the following:

New nido-carborane based carboxylic acids 10-HOOC(CH2)n(Me)S-7,8-C2B9H11 (n = 1-4) were prepared by alkylation of Bu4N salt of 10-methylthio-7,8-dicarba-nido-borane with ω-haloalkyl esters or nitriles followed by acid hydrolysis. Likewise nido-carborane based amines 10-H2N(CH2)n(Me)S-7,8-C2B9H11 (n = 2, 3) were obtained using ω-bromoalkylphthalimides as alkylating agents followed by removal of the protecting group with hydrazine. Structure of 10-C6H4(CO)2NCH2CH2(Me)S-7,8-C2B9H11 was determined by single crystal x-ray diffraction. 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 amine carboranylthioalkyl derivative preparation, carboxylic acid carboranylthioalkyl derivative preparation, carboranyl thioalkylphthalimide preparation crystal structure reaction hydrazine, mol structure carboranyl thioalkylphthalimide, alkylation thiodicarbaborane haloalkyl ester nitrile and other aspects.COA of Formula: C10H8BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 14, 2022, Kuduk, Scott; Pietsch, Eva Christine; Guttke, Christina D.; Bush, Tammy L. published a patent.Related Products of 1003709-39-4 The title of the patent was Preparation of substituted isoquinolinones as dihydroorotate dehydrogenase inhibitors for use in combinations with hypomethylating agents. And the patent contained the following:

Disclosed are methods of treating a subject who has been diagnosed with a disease, syndrome, condition, or disorder affected by DHODH enzymic activity comprising administering: a therapeutically effective amount of a DHODH inhibitor I [X = CH or N; Y = CH or N; R1 = (un)substituted alkyl, haloalkyl, cycloalkyl, etc.; R2 = II (wherein Ra = alkyl, haloalkyl, cycloalkyl; Rb = (un)substituted alkyl); R3 = H, halo, Me and OMe; R4 = (un)substituted alkyl, cycloalkyl, pyridyl, etc.], a therapeutically effective amount of a hypomethylating agent and optionally, a therapeutically effective amount of a BCL-2 inhibitor. E.g., a multi-step synthesis of III, starting from Et 2-(benzyloxy)acetate and hydrazine hydrate, was described. The latter was assessed for its ability to induce cytotoxicity in 30 primary AMF patient samples by Cell TiterGlo assay. Eighteen of the AMF samples were highly sensitive to the compound III resulting in IC50 values between 0.11 and 95.1 nM, one patient sample had an IC50 value of 469.1 nM and the remaining 11 cases demonstrated little sensitivity to III with the highest concentration evaluated (3000 nM) unable to kill more than 50% of the tumor cells. The experimental process involved the reaction of 2-Bromo-4-fluoro-5-methylbenzoic acid(cas: 1003709-39-4).Related Products of 1003709-39-4

The Article related to isoquinolinone preparation dihydroorotate dehydrogenase inhibitor combination chemotherapy hypomethylating agent, dhodh inhibitor combination chemotherapy hypomethylating agent isoquinolinone preparation, combination chemotherapy dhodh bcl2 inhibitor hypomethylating agent isoquinolinone preparation and other aspects.Related Products of 1003709-39-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On February 7, 2018, Neuzil, Jiri; Werner, Lukas; Stursa, Jan published a patent.Application of 83152-22-1 The title of the patent was Triphenylphosphonium biguanide analogs, the method of their preparation and their use as a medication. And the patent contained the following:

Biguanides R5R4NC(:NR6)NR3C(:NR7)NR1R2·HX (1, R1-R7 = H, C1-6 alkyl, aralkyl, or substituent ZPPh3+Y-, where Z = linear C2-C20 alkylene, preferably, C8-12 alkylene), useful as antidiabetic agents, for treatment of Diabetes mellitis type II, and diabetes-induced tumors, were prepared by quaternization of PPh3 with 1,ω-dihaloalkanes XZX (2, X = halo), amination of resulting haloalkylphosphonium salts XZPPh3+X- with ammonia or primary amines R1NH2 and reaction with cyanoguanidines R5R4NC(:NR6)NCN. The prepared compounds 1 were examined for growth inhibition and apoptosis of pancreatic cell lines, for suppression of mitochondrial respiration through inhibition of complex I and increase of production of ROS. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).Application of 83152-22-1

The Article related to biguanide phosphonium salt derivative preparation antidiabetic antitumor agent, pancreatic tumor cell line inhibition biguanide phosphonium salt, mitochondrial respiration inhibition tumor cell line biguanide phosphonium salt, reactive oxygen species generation tumor cell line biguanide phosphonium and other aspects.Application of 83152-22-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Turksoy, Abdurrahman; Scattolin, Thomas; Bouayad-Gervais, Samir; Schoenebeck, Franziska published an article in 2020, the title of the article was Facile Access to AgOCF3 and Its New Applications as a Reservoir for OCF2 for the Direct Synthesis of N-CF3, Aryl or Alkyl Carbamoyl Fluorides.Safety of 4-(Bromomethyl)-1,1′-biphenyl And the article contains the following content:

Herein, a straightforward and quant. strategy for the preparation of valuable AgOCF3 at room temperature and showcase its performance in trifluoromethoxylations or as reservoir for O=CF2 was showed. This enabled the direct, practical and safe synthesis of valuable N-alkyl/aryl carbamoyl fluorides and N-CF3 carbamoyl fluorides from secondary amines and isothiocyanides, resp. Mechanistic data indicated that AgOCF3 does not liberate O=CF2 until it was activated by a nucleophilic co-reagent, reinforcing the stability of the salt under new preparation strategy. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Safety of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to silver trifluoromethoxide green preparation, trifluoromethyl ether preparation, alkyl halide silver trifluoromethoxide substitution, alc alkyl silver trifluoromethoxide dehydrotrifluoromethoxylation, carbamoyl fluoride preparation, n-trifluoromethyl, carbamoyl fluorides, fluorination, mechanism, synthetic methods and other aspects.Safety of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 22, 1999, Stolle, Andreas; Antonicek, Horst-Peter; Lensky, Stephen; Voerste, Arnd; Muller, Thomas; Baumgarten, Jorg; Von Dem Bruch, Karsten; Muller, Gerhard; Stropp, Udo; Horvath, Ervin; De Vry, Jean-Marie Viktor; Schreiber, Rudy published a patent.SDS of cas: 259231-26-0 The title of the patent was Preparation of 6-benzyl-5-methylidenehexahydrocyclopenta[c]furan-1-ones as metabotropic glutamate receptor modulators.. And the patent contained the following:

Title compounds [I; A = CH2, CO, CR4OH, (CH2)aCHR5, alkylene, alkenylene, alkynylene; a = 0-4; R4 = H, alkyl; R5 = Ph; R1 = H, (substituted) cycloalkyl, heterocyclyl, benzoheterocyclyl, aryl, etc.; R2, R3 = H, alkyl; DE = CH2C(:CR32R31)CH2, CR33:CR34CHR35, etc.; R31-R35 = H, Ph, alkyl], were prepared for preventing and/or treating diseases caused by the hyper- or hypofunction of the glutamatergic system, especially cerebral ischemia, cranial/cerebral trauma, pain or CNS-mediated cramps (no data). Thus, 2-methoxycarbonyl-4-methylidenecyclopentanecarboxylic acid in THF at -15° was treated with Et3n and EtO2CCl followed by 1 h stirring at room temperature The mixture was filtered and the filtrate in MeOH at -15° was treated with NaBH4 followed by 1 h stirring at room temperature to give 58% (3aS*,6aR*)-5-methylidenehexahydrocyclopenta[c]furan-1-one. The latter in PhMe was was added to LiN(SiMe3)2 in THF/PhMe at -78° followed by warming to room temperature, 1 h stirring, and addition of PhCH2Br to give 68% (3aS*,6aR*)-6a-benzyl-5-methylidenehexahydrocyclopenta[c]furan-1-one. The experimental process involved the reaction of 2-Bromo-4-(bromomethyl)-1-methylbenzene(cas: 259231-26-0).SDS of cas: 259231-26-0

The Article related to benzylmethylidenehexahydrocyclopentafuranone preparation metabotropic glutamate receptor modulator, cyclopentafuranone benzyl methylidene preparation metabotropic glutamate receptor modulator, analgesic benzylmethylidenehexahydrocyclopentafuranone, head trauma treatment benzylmethylidenehexahydrocyclopentafuranone and other aspects.SDS of cas: 259231-26-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 10, 2009, Fukuoka, Masayoshi; Yokogawa, Tatsushi; Miyahara, Seiji; Miyakoshi, Hitoshi; Yano, Wakako; Taguchi, Junko; Takao, Yayoi published a patent.Application of 1187931-17-4 The title of the patent was Preparation of novel uracil compounds having inhibitory activity on human deoxyuridine triphosphatase or salts thereof. And the patent contained the following:

There are disclosed uracil compounds or salts thereof which have an excellent inhibitory activity on human deoxyuridine triphosphatase (dUTPase) and are useful as therapeutic agents for treating diseases caused by dUTPase, e.g. as anti-tumor agents. There are specifically disclosed uracil compounds represented by general formula [I; n = 1-3 integer; X = a bond, O, S, C2-6 alkenylene, (un)substituted divalent aromatic hydrocarbon group, (un)substituted and (un)saturated divalent heterocyclic group; Y = a bond, C1-8 linear or branched alkylene optionally having cycloalkylidene structure on one of the carbon atoms; Z = SO2NR1R2, NR3SO2R4; R1, R2 = C1-6 alkyl, (un)substituted aralkyl wherein in case where the aromatic hydrocarbon group of the aralkyl is Ph, the Ph and its substituents together form a condensed bicyclic hydrocarbon group; or NR1R2 form (un)substituted saturated heterocyclic ring; R3 = H, C1-6 alkyl; R4 = each (un)substituted aromatic hydrocarbon group or unsaturated heterocyclic group] or salts thereof. Thus, 6.8 g N-(3-(cyclopropylmethoxy)benzyl)-3-(methoxymethoxy)propane-1-sulfonamide was dissolved in 20 mL CH2Cl2, treated with a solution of 6.7 mL 1.0 M BCl3/CH2Cl2 at 0°, stirred at room temperature for 1.5 h, concentrated under reduced pressure, redissolved in 25 mL CH2Cl2, treated with a solution of 7.1 g 2,4-bis(trimethylsilyloxy)pyrimidine in 150 mL CH2Cl2 and 180 mg iodine, and heated at reflux for 95° for 3.5 h to give, after workup and silica gel chromatog., 42% N-(3-(cyclopropylmethoxy)benzyl)-3-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)propane-1-sulfonamide (II). II and (R)-N-(1-(3-(cyclopropylmethoxy)-4-fluorophenyl)propyl)-3-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)propane-1-sulfonamide (III) showed IC50 of 0.33 and 0.03 μM, resp., against human deoxyuridine triphosphatase. The experimental process involved the reaction of (R)-1-(2-Bromophenyl)ethanamine hydrochloride(cas: 1187931-17-4).Application of 1187931-17-4

The Article related to antitumor uracil derivative preparation, sulfonamide containing uracil derivative preparation inhibitor human deoxyuridine triphosphatase, uracil derivative preparation inhibitor human deoxyuridine triphosphatase, dioxodihydropyrimidinylmethoxypropanesulfonamide preparation inhibitor human deoxyuridine triphosphatase and other aspects.Application of 1187931-17-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 15, 2007, Ju-Nam, Yon; Allen, David W.; Gardiner, Philip H. E.; Light, Mark E.; Hursthouse, Michael B.; Bricklebank, Neil published an article.Reference of (6-Bromohexyl)triphenylphosphonium bromide The title of the article was The synthesis and characterisation of masked phosphonioalkyl selenolates: Potential ligands for the production of functionalised gold nanoparticles. And the article contained the following:

Two new masked phosphonioalkylselenolate ligands, bis(3-triphenylphosphoniopropyl) diselenide- and [6-(selenocyanato)hexyl]triphenylphosphonium selenocyanates, were prepared The mol. structure of the bis(3-triphenylphosphoniopropyl) diselenide diselenocyanate was determined by x-ray crystallog. The structure reveals an overall stoichiometry of {[Ph3P+(CH2)3Se]2(SeCN-)2·KOH}, with the bis(3-triphenylphosphoniopropylselenium) diselenocyanate units arranged in pairs around an inversion center. The K ion is disordered over several positions but its main component forms a near linear K···Se contact to one of the Se atoms in the diselenide bond. The hexyl derivative, [6-(selenocyanato)hexyl]triphenylphosphonium selenocyanate forms as a yellow oil that was characterized spectroscopically. Both phosphonioalkylselenide cations undergo reductive cleavage to form phosphonioalkylselenolate zwitterions. Attempts to prepare phosphonioalkylselenolate-functionalized Au nanoparticles in situ through the NaBH4-promoted reduction of tetrachloroaurate salts in a H2O/CH2Cl2 biphasic system gave colloidal gold. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).Reference of (6-Bromohexyl)triphenylphosphonium bromide

The Article related to gold nanoparticle attempted stabilization phosphoniopropyl diselenide selenocyanatohexylphosphonium selenocyanate, phosphoniopropyl diselenide selenocyanate preparation structure reduction attempted nanoparticle stabilization, selenocyanatohexylphosphonium selenocyanate preparation attempted gold nanoparticle stabilization and other aspects.Reference of (6-Bromohexyl)triphenylphosphonium bromide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 7, 2021, Zhang, Shuai; Xiao, Jun-Zhao; Li, Yan-Bo; Shi, Chang-Yun; Yin, Liang published an article.Synthetic Route of 2567-29-5 The title of the article was Copper(I)-Catalyzed Asymmetric Alkylation of Unsymmetrical Secondary Phosphines. And the article contained the following:

A Cu(I)-catalyzed asym. alkylation of HPAr1Ar2 with alkyl halides is uncovered, which provides an array of P-stereogenic phosphines in generally high yield and enantioselectivity. The electrophilic alkyl halides enjoy a broad substrate scope, including allyl bromides, propargyl bromide, benzyl bromides, and alkyl iodides. Also, 11 unsym. diarylphosphines (HPAr1Ar2) serve as competent pronucleophiles. The present methodol. is also successfully applied to catalytic asym. double and triple alkylation, and the corresponding products were obtained in moderate diastereo- and excellent enantioselectivities. Some 31P NMR experiments indicate that bulky HPPhMes exhibits weak competitively coordinating ability to the Cu(I)-bisphosphine complex, and thus the presence of stoichiometric HPAr1Ar2 does not affect the enantioselectivity significantly. Therefore, the high enantioselectivity in this reaction is attributed to the high performance of the unique Cu(I)-(R,RP)-TANIAPHOS complex in asym. induction. Finally, one monophosphine and two bisphosphines prepared by the present reaction are employed as efficient chiral ligands to afford three structurally diversified Cu(I) complexes, which demonstrates the synthetic utility of the present methodol. 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 chiral benzyldiarylphosphine sulfide preparation crystal structure, crystal structure chiral benzyldiarylphosphine sulfide bisphosphine copper bridging halide, mol structure chiral benzyldiarylphosphine sulfide bisphosphine copper bridging halide, bisphosphine copper bridging halide cage complex preparation crystal structure and other aspects.Synthetic Route of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On November 28, 2019, Takeda, Shigemitsu; Shirahase, Hiroaki; Takashima, Shunsuke; Kitao, Tatsuya published a patent.Synthetic Route of 1160653-94-0 The title of the patent was Preparation of 2H-10-oxa-2-azaanthracene-1,9-dione derivatives as readthrough inducers for premature termination codons and pharmaceutical use thereof. And the patent contained the following:

The present invention pertains to the 2H-10-oxa-2-azaanthracene-1,9-dione compounds (1,2-dihydro-10H-pyrido[4,3-b]chromene-1,10-dione derivatives) represented by general formula I [R1 = (un)substituted ring group; R2 = each (un)substituted C1-6 alkyl, C3-6 cycloalkyl, or C3-8 cycloalkenyl; R3, R4, R5 = each independently H, halo, cyano, hydroxy, or each (un)substituted acyl, NH2, C1-6 alkyl, C1-6 alkoxy, heterocyclyl, or heterocyclyloxy; or R3 and R4 or R4 and R5 are bonded to each other to form each (un)substituted C5-7 cycloalkene or 5- to 7-membered monocyclic nonaromatic heterocyclic ring together with the carbon atoms to which they are bonded]. A pharmaceutical composition containing the compound I or its pharmaceutically acceptable salt as an active ingredient, a readthrough inducer for premature termination codons containing the compound I or its pharmaceutically acceptable salt, and a prophylactic or therapeutic agent containing the compound I or its pharmaceutically acceptable salt as an active ingredient for nonsense mutation genetic disorder are also provided. The nonsense mutation genetic disorder is mucopolysaccharidosis, muscular dystrophy, Duchenne muscular dystrophy, cystic fibrosis, ceroid lipofuscinosis or Niemann-Pick disease. The compounds I or pharmaceutically acceptable salt thereof have readthrough activity for the nonsense mutation that results in premature termination codons, enable the production of full-length proteins, and are useful for the prevention or treatment of the nonsense mutation genetic disorder described above. Thus, 6-cyclobutyl-2-oxo-1-phenyl-1,2-dihydropyridin-4-yl 2-fluorobenzoate was esterified by 2-fluorobenzoyl chloride in the presence of Et3N in toluene at room temperature fro 40 min to quant. give 6-cyclobutyl-2-oxo-1-phenyl-1,2-dihydropyridin-4-yl 2-fluorobenzoate which underwent cyclization by treatment with KCN, Et3N, and 18-crown-6 in toluene at 50° for 4 h to give 43% 3-cyclobutyl-2-phenyl-2H-10-oxa-2-azaanthracene-1,9-dione (II). II at 3 μM increased the activity of α-L-iduronidase 1.5 to -10-times in Hurler syndrome patient-derived fibroblast possessing α-L-iduronidase W402X-mutation. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methoxybenzaldehyde(cas: 1160653-94-0).Synthetic Route of 1160653-94-0

The Article related to nonsense mutation genetic disorder prevention treatment oxaazaanthracenedione preparation, dihydropyridochromenedione oxaazaanthracenedione preparation readthrough inducer premature termination codon, mucopolysaccharidosis muscular dystrophy prevention treatment, duchenne muscular dystrophy cystic fibrosis prevention treatment and other aspects.Synthetic Route of 1160653-94-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary