Tag: 100-200

On January 4, 2007, Ibrahim, Prabha N.; Artis, Dean R.; Bremer, Ryan; Habets, Gaston; Mamo, Shumeye; Nespi, Marika; Zhang, Chao; Zhang, Jiazhong; Zhu, Yong-Liang; Zuckerman, Rebecca; West, Brian; Suzuki, Yoshihisa; Tsai, James; Hirth, Klaus-Peter; Bollag, Gideon; Spevak, Wayne; Cho, Hanna; Gillette, Samuel J.; Wu, Guoxian; Zhu, Hongyao; Shi, Shenghua published a patent.Formula: C7H6F3NO The title of the patent was Pyrrolo[2,3-b]pyridine derivatives as protein kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Compounds of formula I which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Compounds of formula I wherein Q is (un)substituted aryl, (un)substituted indole, (un)substituted heteroaryl, etc.; A is O, S, (un)substituted methylene, NH and derivatives, CO, CS, SO and SO2; R4 – R6 is H, halo, (un)substituted lower alkyl, (un)substituted lower alkenyl, (un)substituted alkynyl, (un)substituted (hetero)cycloalkyl, and (un)substituted (hetero)aryl; and their pharmaceutically acceptable salts, prodrugs, tautomers, and isomers thereof, are claimed. Example compound II was prepared by carboxylation of 2,4-difluoroaniline with benzyl chloroformate; the resulting benzyl 3-amino-2,6-difluorobenzoate underwent sulfonylation with propane-1-sulfonyl chloride to give benzyl 2,6-difluoro-3-(propylsulfonylamino)benzoate, which underwent hydrogenation to give the corresponding benzoic acid, which underwent chlorination, to give the corresponding acid chloride, which underwent reaction with 5-bromo-7-azaindole to give compound II. All the invention compounds were evaluated for their protein kinase inhibitory activity. Several of the tested compounds exhibited good protein kinase inhibitory activity against several kinases. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Formula: C7H6F3NO

The Article related to pyrrolopyridine preparation protein kinase inhibitory activity, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Formula: C7H6F3NO

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On August 4, 2022, Li, Ao; Chen, Yile; Cao, Guoqing published a patent.COA of Formula: C6H10O3 The title of the patent was Toxin molecule suitable for antibody-drug conjugate. And the patent contained the following:

The present invention provides a toxin mol. suitable for an antibody-drug conjugate. In particular, the present invention provides a compound represented by structure I (X = H, OH, NH2, NHR0; Y = (CR1R2)n; Z = bond, carbonyl, thiocarbonyl, sulfonyl, etc.; R0 = C1-8 alkyl, haloalkyl, alkoxy, etc.; R1,R2 = H, D, halo, alkyl, etc.; R3,R4 = halo, C1-8 alkyl, haloalkyl, etc.; n = 0-3 integers). The claimed compound is prepared via multiple steps (procedure given). The prepared compound can be used in the preparation of a pharmaceutical composition for treating diseases associated with tumor cell proliferation. The experimental process involved the reaction of 3-Cyclopropyl-2-hydroxypropanoic acid(cas: 1599840-16-0).COA of Formula: C6H10O3

The Article related to toxin mol preparation antibody drug conjugate antitumor agent, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.COA of Formula: C6H10O3

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On October 29, 2020, Siegel, Stephan; Siegel, Franziska; Schulze, Volker; Berger, Markus; Graham, Keith; Suelzle, Detlev; Boemer, Ulf; Korr, Daniel; Schroeder, Jens; Moenning, Ursula; Niehues, Michael; Meyerson, Matthew; Greulich, Heidi; Kaplan, Bethany published a patent.Synthetic Route of 1620510-51-1 The title of the patent was Preparation of 4H-pyrrolo[3,2-c]pyridin-4-one derivatives as EGFR inhibitors. And the patent contained the following:

Title compounds I [wherein X and Y independently = O or (un)substituted NH; R1 = Me, Et, or CF3, etc.; R2 = H, Me, or Et, etc.; R3 = H or F; R4 = H or Me; R5 = H, CF3, or C1-3 alkyl, etc.; A = (HCR6)n, n is 0 or 1; R6 = H, C1-3 alkyl, or C1-3 haloalkyl], and their pharmaceutically acceptable salts thereof, were prepared as EGFR inhibitors. Thus, the invention compound I (X = Y = O; R1 = OMe; R2 = Cl; R3 = H; R4 = H; R5 = H; A = absence) was prepared and gave a mutEGFR inhibition IC50 value of 1.59E-10 mol/L in D770_N771insSVD kinase assay. The experimental process involved the reaction of (R)-(4-Methylmorpholin-3-yl)methanol(cas: 1620510-51-1).Synthetic Route of 1620510-51-1

The Article related to pyrrolopyridinone antitumor preparation egfr inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Synthetic Route of 1620510-51-1

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On January 4, 2007, Ibrahim, Prahbha N.; Artis, Dean R.; Bremer, Ryan; Mamo, Shumeye; Nespi, Marika; Zhang, Chao; Zhang, Jiazhong; Zhu, Yong-Liang; Tsai, James; Hirth, Klaus-Peter; Bollag, Gideon; Spevak, Wayne; Cho, Hanna; Gillette, Samuel J.; Wu, Guoxiam; Zhu, Hongyao; Shi, Shenghua published a patent.Reference of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Pyrrolo[2,3-b]pyridine derivatives as protein kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Compounds of formula I which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Compounds of formula I wherein Q is (un)substituted (hetero)aryl, and (un)substituted indole; A is O, S, (un)substituted methylene, NH and derivatives, CO, CS, SO and SO2; R4 – R6 are independently H, halo, (un)substituted lower alkyl, (un)substituted lower alkenyl, (un)substituted lower alkynyl, (un)substituted (hetero)cycloalkyl, (un)substituted (hetero)aryl, etc.; and their pharmaceutically acceptable salts, prodrugs, tautomer, and isomers thereof, are claimed. Example compound II was prepared by carboxylation of 2,4-difluoroaniline with benzyl chloroformate; the resulting benzyl 3-amino-2,6-difluorobenzoate underwent sulfonylation with propane-1-sulfonyl chloride to give benzyl 2,6-difluoro-3-(propylsulfonylamino)benzoate, which underwent hydrolysis to give the corresponding benzoic acid, which underwent chlorination and coupling with 5-bromo-7-azaindole to give compound II. All the invention compounds were evaluated for their protein kinase inhibitory activity. Several of the invention compounds exhibited good inhibitory activity against various protein kinases. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Reference of (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to pyrrolopyridine preparation protein kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Reference of (6-(Trifluoromethyl)pyridin-3-yl)methanol

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Alcohol – Wikipedia,
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On May 31, 2021, Swain, Sharada Prasanna; Shri, Om; Ravichandiran, V. published an article.Application In Synthesis of Pentane-1,5-diol The title of the article was Iridium and bis(4-nitrophenyl)phosphoric acid catalysed amination of diol by hydrogen-borrowing methodology for the synthesis of cyclic amine: Synthesis of clopidogrel. And the article contained the following:

The borrowing hydrogen method is an environmentally benign process for the synthesis of amines, as H2O is the side product. A new green process for the amination of diol by [Ir] catalyst and bis(4-nitrophenyl)phosphoric acid for the synthesis of cyclic amine is reported. This method was successfully applied for the synthesis of antiplatelet drug clopidogrel. The experimental process involved the reaction of Pentane-1,5-diol(cas: 111-29-5).Application In Synthesis of Pentane-1,5-diol

The Article related to clopidogrel preparation green, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Application In Synthesis of Pentane-1,5-diol

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On January 19, 2012, Brown, Alan Daniel; Rawson, David James; Storer, Robert Ian; Swain, Nigel Alan published a patent.Recommanded Product: 386704-04-7 The title of the patent was Preparation of sulfonamide derivatives as Nav1.7 inhibitors. And the patent contained the following:

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors I [X = OCH2, CH2O; Het1 = (un)substituted 9-10 membered heteroaryl comprising 1-3 N atoms; R1 = (cyclo)alkyl (optionally substituted by 1-3 F atoms); R2-R4 = H, F, Cl or OMe; R5 = H, CN, F, Cl, etc.] which are potentially useful in the treatment of a wide range of disorders, particularly pain. Over sixty sulfonamides were prepared Thus, reacting 4-[(5-chloro-6-isobutoxypyridin-3-yloxy)methyl]-2,5-difluorobenzoic acid (preparation given) with methanesulfonamide afforded the sulfonamide II.HNEt2. Exemplified sulfonamides were tested for their ability to block the Nav1.7 channel (EIC50 values were provided). Pharmaceutical compositions comprising the title sulfonamide, alone or in combination with other therapeutic agent, were disclosed. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Recommanded Product: 386704-04-7

The Article related to sulfonamide benzamide preparation voltage gated sodium channel nav17 inhibitor, combination chemotherapy nav17 inhibitor sulfonamide amide benzamide preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Recommanded Product: 386704-04-7

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Alcohol – Wikipedia,
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Zhao, Yao; Rui, Jiacheng; Du, Qiang; Chen, Rizhi; Zhan, Ying; Zheng, Xintao; Wu, Xiaojin published an article in 2021, the title of the article was Catalytic base-controlled regiodivergent heteronucleophilic hydrofunctionalization of β,γ-unsaturated amides.Category: alcohols-buliding-blocks And the article contains the following content:

A general catalytic base-controlled regiodivergent nucleophilic hydrofunctionalization of both terminal and internal β,γ-unsaturated amides has been reported. The atom-economical addition of various S/P-based nucleophiles was also exclusively chemoselective. More than 60 branched or linear hetero-substituted aliphatic amides were synthesized from common starting materials under transition-metal-free conditions. Preliminary mechanistic studies are consistent with proposed divergent catalytic cycles. The experimental process involved the reaction of 1-Decanethiol(cas: 143-10-2).Category: alcohols-buliding-blocks

The Article related to branched linear hetero aliphatic amide preparation regioselective chemoselective, unsaturated amide thol phosphine oxide hydrothiolation hydrophosphinylation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Category: alcohols-buliding-blocks

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Trifilenkov, A. S.; Il’in, A. P.; Kravchenko, D. V.; Dorogov, M. V.; Tkachenko, S. E.; Ivashchenko, A. V. published an article in 2005, the title of the article was Liquid-phase parallel synthesis of 4-sulfanylbenzoic acid derivatives.Electric Literature of 72364-46-6 And the article contains the following content:

Combinatorial libraries of substituted 4-sulfanylbenzamides and their derivatives were synthesized on the basis of 4-fluoro-3-nitrobenzoic acid. The procedure for nucleophilic substitution of fluorine by various thiols has been developed; the resulting 4-sulfenyl-3-nitrobenzoic acids were further converted into the corresponding esters and amides. Oxidation of the sulfide fragment with hydrogen peroxide afforded the corresponding sulfones. The experimental process involved the reaction of (2-Fluorophenyl)methanethiol(cas: 72364-46-6).Electric Literature of 72364-46-6

The Article related to benzamide sulfenyl sulfonyl combinatorial synthesis, benzoate sulfenyl sulfonyl combinatorial synthesis, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Electric Literature of 72364-46-6

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On November 26, 2020, Buysse, Ann M.; Nugent, Benjamin M.; Gustafson, Gary D.; Meyer, Stacy T.; Loy, Brian A.; Kister, Jeremy; Gruber, Joseph M.; Jones, David M.; Avila-Adame, Cruz; Wang, Weiwei; Babij, Nicholas; Petkus, Jeff published a patent.SDS of cas: 386704-04-7 The title of the patent was Fungicidal aryl amidines and their preparation. And the patent contained the following:

This disclosure relates to aryl amidines of formula I and their use as fungicides. One embodiment of the disclosure is a use of a compound of formula I, for protection of a plant against attack by a phytopathogenic organism or the treatment of a plant infested by a phytopathogenic organism, comprising the application of a compound of formula I, or a composition comprising the compound to soil, a plant, a part of a plant, foliage, and/or roots. Compounds of formula I wherein R1 is H, (un)substituted C1-8 alkyl, (un)substituted C2-8 alkenyl, (un)substituted C2-8 alkynyl, etc.; R2, R3, R4 and R5 are independently H, halo, CN, NO2, etc.; R6 is H, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, etc.; R6R7 may be taken together to form (un)substituted (un)saturated C1-8 heterocycloalkyl; R7 and R8 are independently H, (un)substituted C1-8 alkyl, (un)substituted C2-8 alkenyl, (un)substituted Ph, etc.; and tautomers thereof, are claimed. Example compound II was prepared by condensation of of 4-methylbenzyl 4-amino-2,5-dimethylbenzoate with N-(dimethoxymethyl)-N-methylethanamine. The invention compounds were evaluated for their fungicidal activity (data given). The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).SDS of cas: 386704-04-7

The Article related to aryl amidine preparation fungicide, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.SDS of cas: 386704-04-7

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Alcohol – Wikipedia,
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On July 14, 2020, Diroll, Benjamin T. published an article.Reference of 1-Decanethiol The title of the article was Ligand-Dependent Tuning of Interband and Intersubband Transitions of Colloidal CdSe Nanoplatelets. And the article contained the following:

Although surface ligands of colloidal nanocrystals are known to adjust the absolute energy levels of valence and conduction bands of semiconductor nanocrystals, they typically have only minor influence on the band gap or effective masses. This changes in nanoplatelets. Ligand exchange of CdSe colloidal nanoplatelets induces large (up to 300 meV) bathochromic shifts of both interband and intersubband transitions. Here, three families of ligands-halides, thiolates, and phosphonates-are used to tune interband transitions, reflecting electron and hole confinement, across visible wavelengths and intersubband transitions, reflecting electron confinement, across the near-IR spectral window. Careful examination shows that delocalization from expansion of the nanoplatelet short axis, which was reported previously, cannot alone explain observed red shifts. Instead, comparison of intersubband, interband, and hole energy levels shows that ligand head group chem. confers specific, idiosyncratic adjustments of the contribution of conduction and valence bands to the observed bathochromic shifts. Phosphonate ligands show the largest band gap reductions but the smallest red shift of intersubband transition energies; halide-exchanged samples displayed smaller reductions in band gap but large red shifts of intersubband transitions; thiolates fall in between. A related specificity is observed in hole states, which implicates ligand-responsive valence band curvature as an addnl. contribution driving optical changes. For nanoplatelets, surface ligand chem. offers not only a tool to adjust the absolute energy level of conduction and valence bands but also an alternative route to preferential electron or hole band engineering that is normally achieved with inorganic shells. The experimental process involved the reaction of 1-Decanethiol(cas: 143-10-2).Reference of 1-Decanethiol

The Article related to cadmium selenide ligand interband intersubband transition colloid nanoplatelet, Radiation Chemistry, Photochemistry, and Photographic and Other Reprographic Processes: Radiation Chemistry and Photochemistry and other aspects.Reference of 1-Decanethiol

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