- Aromatizing olefin metathesis by ligand isolation inside a metal- organic framework
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The aromatizing ring-closing metathesis has been shown to take place inside an extended porous framework. Employing a combination of solvent-assisted linker exchange and postsynthesis modification using olefin metathesis, the noninterpenetrated SALEM-14 was formed and converted catalytically into PAH-MOF-1 with polycyclic aromatic hydrocarbon (PAH) pillars. The metal-organic framework in SALEM-14 prevents "intermolecular" olefin metathesis from occurring between the pillars in the presence of the first generation Hoveyda-Grubbs catalyst, while favoring the production of a PAH, which can be released from the framework under acidic conditions in dimethylsulfoxide.
- Vermeulen, Nicolaas A.,Karagiaridi, Olga,Sarjeant, Amy A.,Stern, Charlotte L.,Hupp, Joseph T.,Farha, Omar K.,Stoddart, J. Fraser
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Read Online
- A practical synthesis of 4-chloro-3-(hydroxymethyl)pyridine by regioselective one-pot lithiation/formylation/reduction of 4-chloropyridine
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4-Chloro-3-(hydroxymethyl)pyridine was prepared and isolated as its hydrochloride in 85% yield from 4-chloropyridine by formylation with dimethylformamide of the corresponding 3-lithium salt, followed by in situ reduction of the resulting 4-chloro-3-formylpyridine through a crossed- Cannizzaro reaction with aqueous formaldehyde.
- Albanese, Domenico,Penso, Michele,Zenoni, Maurizio
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Read Online
- NOVEL PYRAZOLE DERIVATIVE AS ALK5 INHIBITOR AND USES THEREOF
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The present disclosure relates to a novel substituted pyrazole derivative having an effect of inhibiting serine/threonine kinase activity targeting receptor ALK5 of TGF-β, and a pharmaceutical composition including the compound of the present disclosure as an active ingredient may be useful in preventing and/or treating cancers, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, pulmonary diseases, cardiovascular diseases or metabolic diseases, or other diseases associated with a decrease in TGF family signaling activity.
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- Sulfur-containing amino acid feed additive and preparation method thereof
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The invention discloses a sulfur-containing amino acid feed additive and a preparation method thereof, and belongs to the technical field of synthesis of feed additives. The key point of the technicalscheme of the invention is as shown in specification. Compared with the prior art, the sulfur-containing amino acid feed additive has the beneficial effects that the synthetic method is simple, a molecular structure is novel, and can react with nickel ions in a protein target of urease, the urease is inhibited to a certain extent, and the sulfur-containing amino acid feed additive is expected tobe further popularized and used as a composite feed additive.
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Paragraph 0018-0025
(2019/03/25)
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- A 3 - aldehyde -4 - chloro pyridine green preparation method
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The invention discloses a 3 - aldehyde - 4 - chloro pyridine green preparation method, which belongs to the technical field of organic synthesis. Technical proposal of the invention points are: to pyridine as raw materials, the selective chlorination, after the adoption of the salt in the solvent impurities and product of different solubility, can be recrystallized separation, to obtain 4 - chloro pyridine pure product, finally is then subjected to an N, N - dimethyl formamide substitution reaction to obtain the 3 - aldehyde - 4 - chloro pyridine. The invention compared with the prior art has the following advantages: the invention synthetic method is simple, cheap price of raw materials, and is favorable for industrial production.
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Paragraph 0027-0032
(2019/03/25)
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- A 3 - aldehyde -4 - chloro pyridine preparation method
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The invention discloses a 3 - aldehyde - 4 - chloro pyridine of the preparation method, which belongs to the technical field of organic synthesis. Technical proposal of the invention points are: to pyridine as raw materials, the selective chlorination of at first, through the molecular distillation treatment to obtain a pure 4 - chloro pyridine, then in N, N - dimethyl formamide substitution reaction to obtain the 3 - aldehyde - 4 - chloro pyridine. The invention compared with the prior art has the following advantages: the invention synthetic method is simple, cheap price of raw materials, and is favorable for industrial production.
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Paragraph 0025; 0026; 0027; 0028; 0029; 0030
(2019/03/25)
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- HETEROAROMATIC ELECTROPHILES AND METHODS OF USING THEREOF
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Disclosed herein are compounds, compositions, and methods for reactivating or realkylating aged acetylcholinesterase inhibited by or conjugated to the organophosphorus compound. The organophosphorus compound can be a nerve agent. The acetylcholinesterase can be in the central nerve system (CNS) and/or the peripheral nervous system (PNS) of a subject. Accordingly, methods for ameliorating, diminishing, reversing, treating or preventing the toxic effects of an organophosphorus compound in a subject are provided herein. Methods for prophylactic or therapeutic treatment of exposure to an organophosphorus nerve agent are also provided.
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Page/Page column 50; 51
(2018/09/18)
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- NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF
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There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like.)
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- SULFAMATE DERIVATIVE COMPOUND FOR USE IN PREVENTING OR TREATING EPILEPSY
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The present invention relates to a pharmaceutical composition for treating or preventing epilepsy containing a sulfamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention epilepsy comprising administering a sulfamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of epilepsy.
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Page/Page column 211
(2015/06/25)
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- Double palladium-catalyzed synthesis of azepines
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The synthesis of new 5H-pyridobenzazepine and 5H-dipyridoazepine compounds using as key step a palladium-catalyzed amination-cyclization reaction is reported. By choosing an appropriate combination of ligands and reactants under standardized reaction conditions, N- and S-tricyclic products can be prepared in one step from the appropriate stilbenes. Georg Thieme Verlag Stuttgart · New York.
- Bo?inovi?, Nina,Opsenica, Igor,?olaja, Bogdan A.
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supporting information
p. 49 - 52
(2013/02/23)
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- CHEMICAL MOLECULES THAT INHIBIT THE SLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES
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The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.
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- CARBACEPHEM β-LACTAM ANTIBIOTICS
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Carbacephem -lactam antibiotics having structure (I) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar1, Ar2, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 73-74
(2010/04/06)
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- ISOXAZOLO[4,5]PYRIDIN-3-YL-PIPERAZIN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS
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The present invention provides compounds of formula I, having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cogniti
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Page/Page column 7-8
(2010/04/23)
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- CARBACEPHEM β-LACTAM ANTIBIOTICS
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Carbacephem β-lactam antibiotics having the following chemical structures (I) and (II) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, R1, R2 and R3 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 87-88
(2009/05/30)
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- CHEMICAL MOLECULES THAT INHIBIT THE SLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES
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The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.
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Page/Page column 97-98
(2009/09/04)
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- NOVEL COMPOUNDS
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The present invention relates to compounds of formula (I): and processes for preparing them, compositions containing them and their use in treating diseases relating to inappropriate c-Met activity.
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Page/Page column 40
(2008/12/05)
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- Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers
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A series of new N-type (Cav2.2) calcium channel blockers derived from the 'hit' structures 2-(3-bromo-4-fluorophenyl)-3-(2-pyridin-2-ylethyl)thiazolidin-4-one 9 and its 2-[4-(4-bromophenyl)pyridin-3-yl]-3-isobutyl analogue 10 is described. Exte
- Knutsen, Lars J.S.,Hobbs, Christopher J.,Earnshaw, Christopher G.,Fiumana, Andrea,Gilbert, Jenny,Mellor, Sarah L.,Radford, Fleur,Smith, Nichola J.,Birch, Philip J.,Russell Burley,Ward, Stuart D.C.,James, Iain F.
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p. 662 - 667
(2007/10/03)
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- NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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The present invention encompasses compounds of Formula (I); as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.
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Page/Page column 64
(2010/11/08)
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- ACYCLIC HYDRAZIDES AS CANNABINOID RECEPTOR MODULATORS
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The acyclic hydrazides of the invention are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present inventio
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Page/Page column 47
(2010/11/08)
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- Pyridine metallations in the synthesis of triazole based NK-1 antagonists
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Regioselective pyridine metallation chemistry was used to produce N-(3-chloropyridin-4-ylmethyl)-N-methyl-1-(3,5-bis-trifluoromethylbenzyl)-5-phenyl-1H-[1,2,3]triazole-4-carboxamide (9a) and [1-(3,5-bis-trifluoromethyl-benzyl)-5-morpholin-4-yl-1H-[1,2,3]t
- Jeff Thrasher,Hembre, Erik J.,Gardinier, Kevin M.,Savin, Kenneth A.,Hong, Jian Eric,Jungheim, Louis N.
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p. 543 - 547
(2007/10/03)
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- TACHYKININ RECEPTOR ANTAGONISTS
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The present invention relates to selective NK-1 receptor antagonists of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
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- Novel 3beta-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
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The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3- thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.
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Page/Page column 8
(2010/02/11)
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- Design, synthesis, and AMPA receptor antagonistic activity of a novel 6-nitro-3-oxoquinoxaline-2-carboxylic acid with a substituted phenyl group at the 7 position
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We describe the design, synthesis, and biological properties of a novel series of 7-substituted 6-nitro-3-oxoquinoxaline-2-carboxylic acids. After designing, studying the structure-activity relationships, and evaluating the properties of various compounds
- Takano, Yasuo,Shiga, Futoshi,Asano, Jun,Ando, Naoki,Uchiki, Hideharu,Fukuchi, Kazunori,Anraku, Tsuyosi
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p. 5841 - 5863
(2007/10/03)
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- SUBSTITUTED 4-AMINO-1-(PYRIDYLMETHYL)PIPERIDINE AND RELATED COMPOUNDS
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This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.
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- Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
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The invention provides compounds of Formula I: 1where in W is 2These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful to treat diseases or conditions in which α7 is known to be involved.
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- SUBSTITUTED THIAZOLE DERIVATIVES BEARING 3-PYRIDYL GROUPS, PROCESS FOR PREPARING THE SAME AND USE THEREOF
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The present invention provides a pharmaceutical composition having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism, tumor such as breast cancer and the like, more particularly, a steroid C17,20-lyase inhibitor containing a compound represented by the formula: wherein A1 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, one of A2 and A3 is a hydrogen atom, a halogen atom, a C1-4 aliphatic hydrocarbon group optionally having substituents or an optionally esterified carboxyl group, the other of A2 and A3 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, and at least one of A1, A2 and A3 is a 3-pyridyl group optionally having substituents, or a salt thereof or a prodrug thereof.
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Page/Page column 37
(2008/06/13)
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- Synthesis and AMPA receptor antagonistic activity of a novel class of quinoxalinecarboxylic acid with a substituted phenyl group at the C-7 position
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The synthesis and biological properties of a novel class of 7-heterocycle-substituted quinoxalinecarboxylic acids, which bear a substituted phenyl group through a urethane linkage at the C-7 position, are described. One of the synthesized compounds, 15l,
- Takano, Yasuo,Shiga, Futoshi,Asano, Jun,Ando, Naoki,Uchiki, Hideharu,Anraku, Tsuyosi
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p. 3521 - 3525
(2007/10/03)
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- Inhibitors of protein isoprenyl transferases
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Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (a) (b) —C(O)NH—CH(R14)—C(O)OR15, (c) (d) —C(O)NH—CH(R14)—C(O)NHSO2R16 (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4-L6—C(W)—N(R5)—L5—, (e) —L4-L6—S(O)m—N(R5)—L5—, (f) —L4—N(R5)—C(W)—L7-L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
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- Structural features of azidopyridinyl neonicotinoid probes conferring high affinity and selectivity for mammalian α4β2 and Drosophila nicotinic receptors
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The higher toxicity of neonicotinoid insecticides such as N-(6-chloropyridin-3-ylmethyl)-2-nitroiminoimidazolidine (imidacloprid) to insects than mammals is due in large part to target site specificity at the corresponding nicotinic acetylcholine receptors (nAChRs). We propose that neonicotinoids with a protonated N-unsubstituted imine or equivalent substituent recognize the anionic subsite of the mammalian α4β2 nAChR whereas the negatively charged (δ-) tip of the neonicotinoid, insecticides interacts with a putative cationic subsite of the insect nAChR. This hypothesis can be tested by using two photoaffinity probes that differ only in the N-unsubstituted imine vs negatively charged (δ-) tip. Synthesis methodology was developed for compounds combining three moieties: pyridin-3-ylmethyl or 6-chloropyridin-3-ylmethyl and their 4- and 5-azido analogues; imidazolidine, 4-imidazoline or 4-thiazoline; and N-unsubstituted imine, nitroimine, cyanoimine, or nitromethylene. Structure-activity studies compared displacement of [3H] nicotine binding in mammalian α4β2 nAChR and [3H]imidacloprid binding in Drosophila nAChR. Preferred compounds are N-(5-azido-6-chloropyridin-3-ylmethyl) with 2-iminothiazoline for α4β2 (Ki = 0.47 nM) and with 2-nitroiminothiazoline or 2-nitromethyleneimidazolidine for Drosophila (Ki = 0.72-3.9 nM).
- Zhang, Nanjing,Tomizawa, Motohiro,Casida, John E.
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p. 2832 - 2840
(2007/10/03)
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- ENDOTHELIN RECEPTOR ANTAGONISTS
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Novel pyridines, pyrimidines, pyrazines, pyridazines and triazines, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
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- ENDOTHELIN RECEPTOR ANTAGONISTS
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Novel indane and indene derivatives are described which are endothelin receptor antagonists.
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- Directed Lithiation of 4-Halopyridines: Chemoselectivity, Regioselectivity and Application to Synthesis
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4-Chloro and 4-fluoropyridines were ortho-lithiated by n-butyllithium-TMEDA chelate or lithium diisopropylamide at low temperature.The resulting 3-lithio 4-halopyridines were reacted with electrophiles which led to various 3,4-disubstituted pyridines.The versatility of this functionalization is enhanced by the 4-halogen reactivity towards nucleophiles such as water, methylate and amines.Some of the 3,4-disubstituted synthons were annelated to naphthyridine, xanthone and coumarin or condensed to Hantzsch-ester or to "chlotrimazol" analogues.Lithiation of 4-fluoropyridine led in one step to 3,4-pyridyne, which was trapped by cycloaddition with furans.
- Marsais, F.,Trecourt, F.,Breant, P.,Queguiner, G.
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