Tag: M.W=150-200

Hua, Zihao; Huang, Xin; Bregman, Howard; Chakka, Nagasree; DiMauro, Erin F.; Doherty, Elizabeth M.; Goldstein, Jon; Gunaydin, Hakan; Huang, Hongbing; Mercede, Stephanie; Newcomb, John; Patel, Vinod F.; Turci, Susan M.; Yan, Jie; Wilson, Cindy; Martin, Matthew W. published the artcile< 2-(Phenylamino)-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1γ) inhibitors>, HPLC of Formula: 401567-00-8, the main research area is phenylamino cyano benzimidazole preparation casein kinase inhibitor treatment cancer.

Screening of the amgen compound library led to the identification of 2-(phenylamino)-6-cyano-1H-benzimidazole, I, as a potential CK1 gamma inhibitor (CK1γ) with excellent kinase selectivity and unprecedented CK1 isoform selectivity. Further structure-based optimization of this series resulted in the discovery of II, which possessed good enzymic and cellular potency, excellent CK1 isoform and kinase selectivity, and acceptable pharmacokinetic properties.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 401567-00-8 belongs to class imidazoles-derivatives, and the molecular formula is C8H4ClN3, HPLC of Formula: 401567-00-8.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Wang, Xuan; Sun, Hui; Liu, Jiaxiang; Zhong, Wenge; Zhang, Mingqiang; Zhou, Hu; Dai, Dongcheng; Lu, Xiaojie published the artcile< Palladium-Promoted DNA-Compatible Heck Reaction>, Quality Control of 1003-21-0, the main research area is palladium promoted Heck reaction on DNA; DNA conjugated styrene acrylamide aryl iodide single strand DNA.

Optimal conditions for palladium-promoted Heck reaction on DNA were developed with good to excellent conversions. Versatility with either DNA-conjugated styrene/acrylamide or aryl iodide and a broad substrate scope of the corresponding coupling partners were established. Furthermore, robustness of the Heck reaction conditions on single-strand DNA and feasibility for DNA-encoded library production were demonstrated.

Organic Letters published new progress about Amides Role: SPN (Synthetic Preparation), PREP (Preparation). 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Quality Control of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Sakamoto, Takao; Kondo, Yoshinori; Suginome, Takashi; Ohba, Setsuya; Yamanaka, Hiroshi published the artcile< Palladium-catalyzed cross-coupling reaction of haloazoles with phenylsulfonylacetonitrile>, COA of Formula: C4H5BrN2, the main research area is palladium catalyzed cross coupling reaction haloazole; condensation haloazole phenylsulfonylacetonitrile; oxazoleacetonitrile phenylsulfonyl; thiazoleacetonitrile phenylsulfonyl; imidazoleacetonitrile phenylsulfonyl.

Condensation of halo-substituted 1,3-azoles (1,3-oxazoles, 1,3-thiazoles and imidazoles), e.g., I (R = Br), with phenylsulfonylacetonitrile under basic conditions was promoted by the catalytic action of tetrakis(triphenylphosphine)palladium(0) to give α-phenylsulfonyl-1,3-azoleacetonitriles, e.g., I (R = PhO2SCHCN). The adaptability of halogen atoms for the cross-coupling reaction was investigated. The reaction of 4-halo-1,2-azoles was also examined

Synthesis published new progress about Cross-coupling reaction. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, COA of Formula: C4H5BrN2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Ogino, Yoshio; Ohtake, Norikazu; Nagae, Yoshikazu; Matsuda, Kenji; Moriya, Minoru; Suga, Takuya; Ishikawa, Makoto; Kanesaka, Maki; Mitobe, Yuko; Ito, Junko; Kanno, Tetsuya; Ishihara, Akane; Iwaasa, Hisashi; Ohe, Tomoyuki; Kanatani, Akio; Fukami, Takehiro published the artcile< Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4'-piperidin]-1'-yl}benzimidazole derivatives>, HPLC of Formula: 401567-00-8, the main research area is isobenzofuran piperidinyl benzimidazole preparation neuropeptide Y Y5 receptor antagonist; NPY Y Y5 receptor antagonist sar isobenzofuran piperidinyl benzimidazole.

Design, syntheses, and structure-activity relationships of a novel class of 2-{3-oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole NPY Y5 receptor antagonists are described. The benzimidazole structures were newly designed based on the urea linkage of our prototype Y5 receptor antagonists. By optimizing substituents on the benzimidazole core part of the lead compound I (R = H), a potent, orally available, and brain-penetrable Y5 selective antagonist I (R = CF3) was developed.

Bioorganic & Medicinal Chemistry Letters published new progress about Drug design. 401567-00-8 belongs to class imidazoles-derivatives, and the molecular formula is C8H4ClN3, HPLC of Formula: 401567-00-8.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Demetrio da Silva, Vinicius; de Barros, Italo Ribeiro; da Conceicao, Debora K. Silva; de Almeida, Kauana Nunes; Schrekker, Henri Stephan; Amico, Sandro C.; Jacobi, Marly M. published the artcile< Aramid pulp reinforced hydrogenated nitrile butadiene rubber composites with ionic liquid compatibilizers>, Quality Control of 700370-07-6, the main research area is aramid pulp reinforced hydrogenated nitrile butadiene rubber composite compatibilizer.

Although carbon black is an effective reinforcement for most rubbers, its replacement by other fillers would be beneficial. Aramid fibers are used in a range of applications in the rubber industry, providing dimensional stability prior to vulcanization and improving the mech. properties of the elastomeric product. Nevertheless, their relatively inert surface is an obstacle in the exploitation of their full potential. In this work, two ionic liquids were investigated as compatibilizers in the preparation of hydrogenated nitrile butadiene rubber composites with aramid pulp and carbon black fillers. The materials were characterized using swelling, hardness and tensile tests, differential scanning calorimetry, thermal gravimetric anal., and IR spectroscopy. The carbon black-free composite prepared from aramid pulp treated with 1.0 wt% of 1-carboxymethyl-3-methylimidazolium chloride outperformed all other studied materials, presenting a higher modulus at 100% strain (7.31 MPa), while maintaining high strain at break. Thus, ionic liquids were found to potentialize the aramid reinforcement effect in these rubber composites. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019, 137, 48702.

Journal of Applied Polymer Science published new progress about Adhesion, physical, interfacial. 700370-07-6 belongs to class imidazoles-derivatives, and the molecular formula is C6H9ClN2O2, Quality Control of 700370-07-6.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Grimmett, M. R. published the artcile< Product class 3: imidazoles>, Category: imidazoles-derivatives, the main research area is review imidazole preparation cyclization aromatization ring transformation.

A review. Methods for preparing imidazoles are reviewed including cyclization, ring transformations, aromatization and modification of substituents on existing imidazoles.

Science of Synthesis published new progress about Aromatization. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Category: imidazoles-derivatives.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Balaban, I. E.; Pyman, F. L. published the artcile< Bromo derivatives of 1-methylglyoxaline and the constitution of ""chloroxalmethylin"">, HPLC of Formula: 1003-21-0, the main research area is .

Bromination of 18 g. 1-methylglyoxaline in 60 cc. CHCl3 with 36 g. Br in 60 cc. CHCl3 at 5-10° gave 10.4 g. 2,4,5-tribromo-1-methylglyoxaline (I), m. 93-4.5° (Wallach, Ber. 16, 537, gives 88-9°), 0.49 g. (as picrate) of 4,5-dibromo-1-methylglyoxaline (II), m. 79-80°, and 23.3 g. (as picrate) of unchanged base. I.HCl, m. 190-200°, dissociates in H2O. I is recovered to the extent of 90% after heating with 1 mol. Na2SO3 in 20% aqueous solution for 5 hrs., 1% of II also being isolated. II was further prepared by heating 4,5-dibromo-1-methylglyoxaline with Me2SO4 and from (CONHMe)2 and PBr5 (7% and 11% with 1 and 2 mols. PBr5, resp.). II.HCl, crystallizing with 2 H2O, lost in vacuo over H2SO4, and then m. 179°; HNO3 salt, m. 153°; picrate, yellow, m. 148-9°, soluble in 6 parts hot EtOH or 30 parts boiling H2O. Methylation of 4(5)-bromoglyoxaline gives 51% III and 1.5% IV (ratio 34:1), separated by fractional crystallization of the picrates from EtOH. 5-Bromo-1-methylglyoxaline (III), b15 128°, m. 45-6°, deliquescent; HCl salt, needles with 0.5 H2O, lost at 100° and then m. 155°; HNO3 salt, anhydrous prisms, m. 155° (effervescence) soluble in 4 parts boiling H2O; H oxalate salt, needles with 0.5 H2O, lost in vacuo over H2SO4 and then m. 147°; picrate, yellow needles, m. 190°. The 4(?)-sulfonic acid, m. 284°, results in 78% yield; it is soluble in 55 parts boiling H2O, almost insoluble in cold H2O. Heating 0.38 g. of the acid with 5 cc. 30% H2SO4 for 3 hrs. at 170° gave 0.11 g. III (as picrate). The 4-nitro derivative (V) of III (80% yield), m. 180°, soluble in 85 parts boiling H2O; HCl salt, m. 155° and decomposed by H2O. V crystallines unchanged from aqueous picric acid. With aqueous Na2SO3 V yields 4-nitro-1-methylglyoxaline-5-sulfonic acid, m. 254° (decomposition); Na salt, fine needles. Hydrolysis of the acid by heating with 30% H2SO4 gives 4-nitro-1-methylglyoxaline; this establishes the orientation of these bases directly and of IV indirectly. III condenses with HCHO, by heating 6 hrs. at 130°, to give 5-bromo-2-hydroxymethyl-1-methylglyoxaline, m. 143° and soluble in 15 parts boiling H2O (yield, 42%); picrate, yellow needles, m. 165-6°. Reduction with HI and red P gives 1,2-dimethylglyoxaline. Either III or IV, heated with MeI, gives 4(5)-bromo-1,3-dimethylglyoxalinium iodide, m. 202-4°, soluble in 8 parts hot EtOH; distillation at 15 mm. and 235° gave 43% IV and some III. 4-Bromo-1-methylglyoxaline (IV) is an oil; HNO3 salt, prisms, m. 155°, soluble in about 3 parts boiling H2O; picrate, yellow needles, m. 179°, soluble in 7 parts hot EtOH. The 5(?)-sulfonic acid (yield, 77%) crystallines with 1 H2O, m. 256° (decomposition), soluble in 15 parts boiling H2O. The 5-nitro derivative (VI) (yield, 54%), m. 105°, soluble in 40 parts boiling H2O. Methylation of 7 g. 4(5)-bromo-5(4)nitroglyoxaline (VII), gave 1.7 g. VI and 1.4 g. unchanged material. Na2SO3 (20% aqueous solution) reacts with VII to give 4(5)-nitroglyoxaline-5(4)-sulfonic acid, decomposes 300° (yield, 88%); Na salt, fine needles. “”Chloroxalmethylin,”” prepared according to W., gives a HNO3 salt, m. 145° which, heated with concentrated H2SO4 1.5 hrs. at 100°, gives 5-chloro-4-nitro-1-methylglyoxaline, m. 147°, soluble in 40 parts boiling H2O; it is therefore 5-chloro-1-methylglyoxaline.

Journal of the Chemical Society, Transactions published new progress about 1003-21-0. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, HPLC of Formula: 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Iida, Hiroki; Umebayashi, Naofumi; Yashima, Eiji published the artcile< Photoswitchable organocatalysis in acylation of alcohol using dithienylethene-linked azoles>, SDS of cas: 1003-21-0, the main research area is dithienylethene linked azole preparation photoswitchable organocatalyst acylation alc.

Three novel dithienylethenes bearing azole derivatives were synthesized and found to undergo reversible photocyclization of the dithienylethene units upon alternate irradiation with UV and visible light. Among them, the dithienylethene-linked imidazole and N-phenylimidazole exhibited a relatively high organocatalytic activity for the acylation of 2-decanol with acetic anhydride, and the catalytic activity of the dithienylethene-linked imidazole could be switched by reversible photoinduced cyclization/cycloreversion of the dithienylethene unit.

Tetrahedron published new progress about Acylation. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, SDS of cas: 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Garbaccio, Robert M.; Brnardic, Edward J.; Fraley, Mark E.; Hartman, George D.; Hutson, Pete H.; O’Brien, Julie A.; Magliaro, Brian C.; Uslaner, Jason M.; Huszar, Sarah L.; Fillgrove, Kerry L.; Small, James H.; Tang, Cuyue; Kuo, Yuhsin; Jacobson, Marlene A. published the artcile< Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor>, Product Details of C8H4ClN3, the main research area is oxazolo benzimidazole derivative preparation allosteric modulator mGluR2 receptor antipsychotic; GPCR; Oxazolobenzimidazoles; allosteric modulators; hyperlocomotion model; metabotropic glutamate 2 receptor; schizophrenia.

Novel oxazolobenzimidazoles are described as potent and selective pos. allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its phys. and pharmacokinetic properties led to the identification of potent and orally bioavailable compounds (20 and 21) as advanced leads. Compound 20 (TBPCOB) was shown to have robust activity in a PCP-induced hyperlocomotion model in rat, an assay responsive to clin. antipsychotic treatments for schizophrenia.

ACS Medicinal Chemistry Letters published new progress about Antipsychotics. 401567-00-8 belongs to class imidazoles-derivatives, and the molecular formula is C8H4ClN3, Product Details of C8H4ClN3.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Kochergin, P. M. published the artcile< Imidazole series. XV. Reaction products of N,N'-dimethyloxamide with pentahalo phosphorus compounds>, Recommanded Product: 5-Bromo-1-methyl-1H-imidazole, the main research area is .

14660a. Heating 2 kg. PCl5 with 550 g. (CONHMe)2 1-1.5 hrs. at 95-8° (exothermic initially), followed by further 1.6 hrs. after cessation of exothermic reaction, gave 50.6% 1-methyl-5-chloroimidazole, b9 84°, b10 87°, n22D 1.5120 (picrate m. 167-8°), unreacted amide, and 1-methyl-4,5-dichloroimidazole, m. 58.5-59° (picrate m. 130.5-1.5°; HCl salt m. 161-3°; nitrate m. 122°; sulfate m. 83-5°). Similar reaction of 11.6 g. (CONHMe)2 with 91.6 g. PCl5 and 250 ml. POCl3 in 0.5 hr. at 40-50°, then 1.5 hrs. at 100°, gave a low yield of 1-methyl-2,4,5-trichloroimidazole, m. 75.5-6° (petr. ether), 1-methyl-4,5-dichloroimidazole, isolated as the picrate, and 1-methyl-5-chloroimidazole. Heating 104 g. PBr5 with 14 g. (CONHMe)2 2.1 hrs. on a steam bath gave 19.6% 1-methyl-4,5-dibromoimidazole, m. 79-80° (picrate m. 149.5-50.5°), and 1-methyl-5-bromoimidazole, isolated as the picrate, m. 190-1°. Nitration of the mixed crude mono- and dibromo derivatives with mixed acid 2 hrs. at 100° gave 1-methyl-4-nitro-5-bromoimidazole, m. 180-1°. Heating (CONHMe)2 with PBr5 in POCl3 in 1 hr. at 60-70° and 2 hrs. at reflux gave 1-methyl-2,4,5-tribromoimidazole, m. 93-4°, 1-methyl-4,5-dibromoimidazole, and 1-methyl-5-bromoimidazole, isolated as the picrate.

Zhurnal Obshchei Khimii published new progress about Group 15 element halides, phosphorus halides. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Recommanded Product: 5-Bromo-1-methyl-1H-imidazole.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem