Tag: 200-300

On March 31, 2021, Sun, Ji-yun; Kumata, Katsushi; Chen, Zhen; Zhang, Yi-ding; Chen, Jia-hui; Hatori, Akiko; Fu, Hua-long; Rong, Jian; Deng, Xiao-yun; Yamasaki, Tomoteru; Xie, Lin; Hu, Kuan; Fujinaga, Masayuki; Yu, Qing-zhen; Shao, Tuo; Collier, Thomas Lee; Josephson, Lee; Shao, Yi-han; Du, Yun-fei; Wang, Lu; Xu, Hao; Zhang, Ming-rong; Liang, Steven H. published an article.Electric Literature of 1820711-82-7 The title of the article was Synthesis and preliminary evaluation of novel 11C-labeled GluN2B-selective NMDA receptor negative allosteric modulators. And the article contained the following:

Abstract: N-methyl-D-aspartate receptors (NMDARs) play critical roles in the physiol. function of the mammalian central nervous system (CNS), including learning, memory, and synaptic plasticity, through modulating excitatory neurotransmission. Attributed to etiopathol. of various CNS disorders and neurodegenerative diseases, GluN2B is one of the most well-studied subtypes in preclin. and clin. studies on NMDARs. Herein, we report the synthesis and preclin. evaluation of two 11C-labeled GluN2B-selective neg. allosteric modulators (NAMs) containing N,N-dimethyl-2-(1H-pyrrolo[3,2-b]pyridin-1-yl)acetamides for positron emission tomog. (PET) imaging. Two PET ligands, namely [11C]31 and [11C]37 (also called N2B-1810 and N2B-1903, resp.) were labeled with [11C]CH3I in good radiochem. yields (decay-corrected 28% and 32% relative to starting [11C]CO2, resp.), high radiochem. purity (>99%) and high molar activity (>74 GBq/μmol). In particular, PET ligand [11C]31 demonstrated moderate specific binding to GluN2B subtype by in vitro autoradiog. studies. However, because in vivo PET imaging studies showed limited brain uptake of [11C]31 (up to 0.5 SUV), further medicinal chem. and ADME optimization are necessary for this chemotype attributed to low binding specificity and rapid metabolism in vivo. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Electric Literature of 1820711-82-7

The Article related to glun2b receptor neg allosteric modulator pet imaging radiotracer brain, glun2b subunit, nmdars, carbon-11, ionotropic glutamate receptors (iglurs), positron emission tomography (pet) and other aspects.Electric Literature of 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 27, 2003, Delorme, Daniel; Woo, Soon Hyung; Vaisburg, Arkadii; Moradel, Oscar; Leit, Silvana; Raeppel, Stephane; Frechette, Sylvie; Bouchain, Giliane published a patent.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine The title of the patent was Preparation of triazinyl and other carboxamides as inhibitors of histone deacetylase. And the patent contained the following:

The invention relates to triazines (shown as I; variables defined below; e.g. 4-[[4-amino-6-(2-indanylamino)-[1,3,5]triazin-2-ylamino]methyl]-N-(2-aminophenyl)benzamide) and Cy3-X1-Ar2-(C(R5):C(R6))qC(O)NH-Ay2 (II; variables defined below; e.g. ), many of which are N-(o-aminophenyl)carboxamides, as inhibitors of histone deacetylase (data included for many I and II). The invention provides compounds and methods for inhibiting histone deacetylase enzymic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. Antineoplastic effects of some I and II are illustrated for colorectal, pulmonary and pancreatic neoplasms; also the combined antineoplastic effect of histone deacetylase inhibitors and histone deacetylase antisense oligonucleotides on tumor cells in vivo was demonstrated. For I: R3 and R4 = H, L1, Cy1 and -L1-Cy1 (L1 = C1-C6 alkyl, C2-C6 heteroalkyl, or C3-C6 alkenyl; Cy1 = cycloalkyl, aryl, heteroaryl, or heterocyclyl) or R3 and R4 are taken together with the adjacent N atom to form a 5-, 6-, or 7-membered ring, wherein the ring atoms = C, O, S, and N, and wherein the ring is optionally substituted, and optionally forms part of a bicyclic ring system, or is optionally fused to one or two aryl or heteroaryl rings, or to one or two saturated or partially unsaturated cycloalkyl or heterocyclic rings, each of which rings and ring systems is optionally substituted. Y1 = -N(R1)(R2), -CH2-C(O)-N(R1)(R2), halogen, and H (R1 and R2 = H, L1, Cy1, and -L1-Cy1). Y2 = chem. bond or N(R0) (R0 = H, alkyl, aryl, aralkyl, and acyl); Ak1 = C1-C6 alkylene, C1-C6-heteroalkylene (preferably, in which one -CH2- is replaced with -NH-, and more preferably -NH-CH2), C2-C6 alkenylene or C2-C6 alkynylene; Ar1 = arylene or heteroarylene, either of which is optionally substituted; and Z1 = C(O)NH-Ay1 and CH:CHC(O)NH-Ay1 (Ay1 = aryl or heteroaryl, each of which is optionally substituted). For II: Cy2 = cycloalkyl, aryl, heteroaryl, or heterocyclyl; X1 = covalent bond, M1-L2-M1, and L2-M2-L2 (L2 = chem. bond, C1-C4 alkylene, C2-C4 alkenylene, and C2-C4 alkynylene, provided that L2 is not a chem. bond when X1 is M1-L2-M1; M1 = -O-, -N(R7)-, -S-, -S(O)-, S(O)2-, -S(O)2N(R7)-, -N(R7)S(O)2-, -C(O)-, -C(O)NH-, -NHC(O)-, -NHC(O)-O- and -OC(O)NH- (R7 = H, alkyl, aryl, aralkyl, acyl, heterocyclyl, and heteroaryl); and M2 = M1, heteroarylene, and heterocyclylene, either of which rings is optionally substituted). Ar2 = arylene or heteroarylene, each of which is optionally substituted; R5 and R6 = H, alkyl, aryl, and aralkyl; q is 0 or 1; and Ay2 is a 5-6 membered cycloalkyl, heterocyclyl, or heteroaryl substituted with an amino or hydroxy moiety (preferably these groups are ortho to the amide N to which Ay2 is attached) and further optionally substituted; provided that when Cy2 is naphthyl, X1 is -CH2-, Ar2 is Ph, R5 and R6 are H, and q is 0 or 1, Ay2 is not Ph or o-hydroxyphenyl. Although the methods of preparation are not claimed, hundreds of example preparations are included. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to carboxamide preparation inhibitor histone deacetylase proliferative disease treatment, triazinyl carboxamide preparation inhibitor histone deacetylase proliferative disease treatment and other aspects.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 4, 2021, Tanaka, Jin; Nagashima, Yuki; Araujo Dias, Antonio Junio; Tanaka, Ken published an article.Formula: C17H20BNO2 The title of the article was Photo-Induced ortho-C-H Borylation of Arenes through In Situ Generation of Rhodium(II) Ate Complexes. And the article contained the following:

Photoinduced in situ “oxidation” of half-sandwich metal complexes to “high-valent” cationic metal complexes has been used to accelerate catalytic reactions. Here, we report the unprecedented photoinduced in situ “reduction” of half-sandwich metal [Rh(III)] complexes to “low-valent” anionic metal [Rh(II)] ate complexes, which facilitate ligand exchange with electron-deficient elements (diboron). This strategy was realized by using a functionalized cyclopentadienyl (CpA3) Rh(III) catalyst we developed, which enabled the basic group-directed room temperature ortho-C-H borylation of arenes. The experimental process involved the reaction of 2-(2-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)pyridine(cas: 1349171-28-3).Formula: C17H20BNO2

The Article related to photocatalyzed regioselective borylation arene rhodium ate in situ catalyst, mol structure optimized rhodium complex transition state potential energy, half sandwich rhodium ate complex in situ catalyst borylation and other aspects.Formula: C17H20BNO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 12, 2000, Ankersen, Michael; Stidsen, Carsten Enggaard; Crider, Michael Albert published a patent.Quality Control of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine The title of the patent was Use of pyridinylaminoalkyl- and imidazolylalkyl-substituted thioureas, isothioureas, and guanidines as somatostatin agonists and antagonists, for treating diseases related to the eye. And the patent contained the following:

The invention relates to the use of somatostatin receptor ligands of nonpeptide origin, e.g., I or II, or a pharmaceutically acceptable salt thereof [wherein: m = 2, 3, 4, 5 or 6; n = 1, 2 or 3; p = 1, 2, 3, 4, 5 or 6; R1, R2 = independently H or C1-6 alkyl optionally substituted with halo, amino, OH, alkoxy, or aryl; X = S, O, NH, NCOPh or N(CN); A = (hetero)aryl optionally substituted with halo, amino, OH, NO2, C1-6 alkyl, C1-6 alkoxy, or aryl, B = (hetero)aryl optionally substituted with halo, amino, OH, C1-6 alkyl, C1-6 alkoxy, or aryl; D = (hetero)aryl or amino, optionally substituted with halo, amino, OH, C1-6 alkyl, C1-6 alkoxy, or aryl]. The compounds have high and/or selective affinity to the somatostatin receptor protein designated SSTR4, and are useful for the preparation of medicaments for treatment of diseases associated with adverse conditions of the retina and/or iris-ciliary body in mammals (no data). Such conditions include high intraocular pressure (IOP) and/or deep ocular infections. The diseases which may be treated are, e.g. glaucoma, stromal keratitis, iritis, retinitis, cataract, and conjunctivitis. Over 40 compounds are claimed for usage, and 27 synthetic examples are given. For instance, propane-1,3-diamine underwent a sequence of: (1) N-arylation with 2-bromopyridine (76%); (2) N-benzylation with NaH and 4-bromobenzyl bromide in DMSO (70%); (3) conversion of the N’-amine to an isothiocyanate using DCC and CS2 (88%); (4) amination of the isothiocyanate with 3-[1-(triphenylmethyl)imidazol-4-yl]propylamine (80%); and (5) deprotection of the trityl group with aqueous HCl in EtOH (99%), to give title compound III.2HCl. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Quality Control of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to thiourea isothiourea guanidine pyridinylaminoalkyl imidazolylalkyl preparation somatostatin agonist antagonist, antiglaucoma somatostatin receptor agonist antagonist thiourea isothiourea guanidine preparation and other aspects.Quality Control of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 4, 2021, Tanaka, Jin; Nagashima, Yuki; Araujo Dias, Antonio Junio; Tanaka, Ken published an article.Formula: C17H20BNO2 The title of the article was Photo-Induced ortho-C-H Borylation of Arenes through In Situ Generation of Rhodium(II) Ate Complexes. And the article contained the following:

Photoinduced in situ “oxidation” of half-sandwich metal complexes to “high-valent” cationic metal complexes has been used to accelerate catalytic reactions. Here, we report the unprecedented photoinduced in situ “reduction” of half-sandwich metal [Rh(III)] complexes to “low-valent” anionic metal [Rh(II)] ate complexes, which facilitate ligand exchange with electron-deficient elements (diboron). This strategy was realized by using a functionalized cyclopentadienyl (CpA3) Rh(III) catalyst we developed, which enabled the basic group-directed room temperature ortho-C-H borylation of arenes. The experimental process involved the reaction of 2-(2-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)pyridine(cas: 1349171-28-3).Formula: C17H20BNO2

The Article related to photocatalyzed regioselective borylation arene rhodium ate in situ catalyst, mol structure optimized rhodium complex transition state potential energy, half sandwich rhodium ate complex in situ catalyst borylation and other aspects.Formula: C17H20BNO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 12, 2000, Ankersen, Michael; Stidsen, Carsten Enggaard; Crider, Michael Albert published a patent.Quality Control of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine The title of the patent was Use of pyridinylaminoalkyl- and imidazolylalkyl-substituted thioureas, isothioureas, and guanidines as somatostatin agonists and antagonists, for treating diseases related to the eye. And the patent contained the following:

The invention relates to the use of somatostatin receptor ligands of nonpeptide origin, e.g., I or II, or a pharmaceutically acceptable salt thereof [wherein: m = 2, 3, 4, 5 or 6; n = 1, 2 or 3; p = 1, 2, 3, 4, 5 or 6; R1, R2 = independently H or C1-6 alkyl optionally substituted with halo, amino, OH, alkoxy, or aryl; X = S, O, NH, NCOPh or N(CN); A = (hetero)aryl optionally substituted with halo, amino, OH, NO2, C1-6 alkyl, C1-6 alkoxy, or aryl, B = (hetero)aryl optionally substituted with halo, amino, OH, C1-6 alkyl, C1-6 alkoxy, or aryl; D = (hetero)aryl or amino, optionally substituted with halo, amino, OH, C1-6 alkyl, C1-6 alkoxy, or aryl]. The compounds have high and/or selective affinity to the somatostatin receptor protein designated SSTR4, and are useful for the preparation of medicaments for treatment of diseases associated with adverse conditions of the retina and/or iris-ciliary body in mammals (no data). Such conditions include high intraocular pressure (IOP) and/or deep ocular infections. The diseases which may be treated are, e.g. glaucoma, stromal keratitis, iritis, retinitis, cataract, and conjunctivitis. Over 40 compounds are claimed for usage, and 27 synthetic examples are given. For instance, propane-1,3-diamine underwent a sequence of: (1) N-arylation with 2-bromopyridine (76%); (2) N-benzylation with NaH and 4-bromobenzyl bromide in DMSO (70%); (3) conversion of the N’-amine to an isothiocyanate using DCC and CS2 (88%); (4) amination of the isothiocyanate with 3-[1-(triphenylmethyl)imidazol-4-yl]propylamine (80%); and (5) deprotection of the trityl group with aqueous HCl in EtOH (99%), to give title compound III.2HCl. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Quality Control of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to thiourea isothiourea guanidine pyridinylaminoalkyl imidazolylalkyl preparation somatostatin agonist antagonist, antiglaucoma somatostatin receptor agonist antagonist thiourea isothiourea guanidine preparation and other aspects.Quality Control of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Thongpaen, Jompol; Schmid, Thibault E.; Toupet, Loic; Dorcet, Vincent; Mauduit, Marc; Basle, Olivier published an article in 2018, the title of the article was Directed ortho C-H borylation catalyzed using Cp*Rh(III)-NHC complexes.Computed Properties of 1349171-28-3 And the article contains the following content:

Cp*Rh(NHC) complexes I(R = iBu, iPr, Me), derived from L-amino acids, with bulky chiral bidentate NHC-carboxylate ligands were efficiently synthesized and fully characterized including solid-state structures. These unprecedented rhodium(III) complexes demonstrated high selectivity in pyridine-directed ortho-C-H borylation of arenes under mild conditions. The experimental process involved the reaction of 2-(2-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)pyridine(cas: 1349171-28-3).Computed Properties of 1349171-28-3

The Article related to directed borylation arylpyridine rhodium chiral nhc catalyst preparation phenol, phenol preparation pyridyl directed borylation oxidation rhodium nhc catalyst, crystal structure rhodium chiral nhc carboxylate half sandwich complex, mol structure rhodium chiral nhc carboxylate half sandwich complex and other aspects.Computed Properties of 1349171-28-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rieder, Samuel; Melendez, Camilo; Denes, Fabrice; Jangra, Harish; Mulliri, Kleni; Zipse, Hendrik; Renaud, Philippe published an article in 2021, the title of the article was Radical chain monoalkylation of pyridines.SDS of cas: 908267-63-0 And the article contains the following content:

The monoalkylation of N-methoxypyridinium salts with alkyl radicals generated from alkenes (via hydroboration with catecholborane), alkyl iodides (via iodine atom transfer) and xanthates to afford alkylated quinoline derivatives R-R1 [R = 4-methylquinolinyl, 4-Cl-quinolinyl, 3-Br-quinolinyl, etc.; R1 = Et, iPr, cyclohexyl, etc.] and pyridine derivatives R2-R3 [R2 = 4-phenylpyridinyl, 4-tBu-pyridinyl, 4-Br-pyridinyl, etc.; R3 = iPr, 1-adamantyl, cyclohexyl, etc.] was reported. The reaction proceeded under neutral conditions since no acid was needed to activate the heterocycle and no external oxidant was required. A rate constant for the addition of a primary radical to N-methoxylepidinium >107 M-1 s-1 was exptl. determined This rate constant was more than one order of magnitude larger than the one measured for the addition of primary alkyl radicals to protonated lepidine demonstrating the remarkable reactivity of methoxypyridinium salts toward radicals. The reaction was used for the preparation of unique pyridinylated terpenoids and was extended to a three-component carbopyridinylation of electron-rich alkenes including enol esters, enol ethers and enamides. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).SDS of cas: 908267-63-0

The Article related to alkylated pyridine derivative preparation, pyridine derivative alkene monoalkylation, alkyl iodide pyridine derivative monoalkylation, xanthate pyridine derivative monoalkylation, derivative pyridine alkylated preparation, ester alkene pyridine derivative three component carbopyridinylation and other aspects.SDS of cas: 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 29, 2015, Basinger, Jillian; Bookser, Brett; Chen, Mi; Chung, Demichael; Gupta, Varsha; Hudson, Andrew; Kaplan, Alan; Na, James; Renick, Joel; Santora, Vincent published a patent.Related Products of 908267-63-0 The title of the patent was Preparation of substituted 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine compounds as GlyT1 inhibitors. And the patent contained the following:

The title compounds I [R1 = CO2H, C(O)NH2, SO2(alkyl), etc.; R2 = H, halo, alkyl, etc.; R3 = H, alkyl, haloalkyl, etc.; R4 = H, F, alkyl, etc.; R5 = alkyl, haloalkyl, alkoxy, etc.; X = (CR)1-2; R = H, alkyl], useful in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurol. disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alc.-dependence, were prepared E.g., a multi-step synthesis of II, starting from tert-Bu 4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate and 1-fluoro-4-iodobenzene, was described. The exemplified compounds I were their GlyT1 inhibitory activity (data given). Pharmaceutical composition comprising I is disclosed. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Related Products of 908267-63-0

The Article related to pyrrolopyrazole pyrazolopyridine preparation glyt1 inhibitor neurol disorder treatment, cns agent cognition enhancer neuroprotection pyrrolopyrazole pyrazolopyridine preparation glyt1, dementia neurodegenerative disease stroke motor deficit pyrrolopyrazole pyrazolopyridine preparation and other aspects.Related Products of 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On May 7, 1998, Ankersen, Michael; Dorwald, Florenzio Zaragoza; Stidsen, Carsten Enggaard; Crider, Albert Michael published a patent.Product Details of 199522-66-2 The title of the patent was Preparation of thiourea derivatives and related compounds as constrained somatostatin agonists and antagonists. And the patent contained the following:

The title compounds B(CH2)nNA(CH2)mYNR1C(:X)E [I; A = (un)substituted aryl; B = (un)substituted aryl; E = heterocyclyl, amino; R1 = H, (un)substituted C1-6 alkyl; X = S, O, NR3; R3 = H, COPh, cyano; Y = bond, etc.; m = 0-6; n = 0-3], somatostatin agonists and antagonists (no data) useful for treating medical disorders related to binding to human somatostatin receptor subtypes, and their pharmaceutically acceptable salts were prepared and claimed. For example, amination of 2,5-dibromopyridine with H2NCH2CH2NH2 in pyridine gave N-1-(5-bromopyrid-2-yl)ethane-1,2-diamine which was benzylated with 3,4-dichlorobenzyl chloride in DMSO in the presence of NaH and the product condensed with CS2 in the presence of dicyclohexylcarbodiimide in THF to give 2-[N-(5-bromopyrid-2-yl)-N-(3,4-dichlorobenzyl)]aminoethyl isothiocyanate. Addition of the latter with 4-[4(5)-imidazolyl]piperidine-2HCl in THF in the presence of Et3N gave a title compound I. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Product Details of 199522-66-2

The Article related to thiourea derivative preparation somatostatin agonist, imidazolylpiperidinecarbothioic acid bromopyridinyldichlorobenzylaminoethylamide, ethanediamine amination dibromopyridine somatostatin agonist preparation, bromopyridylethanediamine preparation benzylation dichlorobenzyl chloride and other aspects.Product Details of 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem