- PHENYLPYRAZOLE COMPOUND AND METHOD FOR CONTROLLING PLANT DISEASE
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The present invention provides a method for controlling a plant disease which comprises applying a compound represented by formula (I) [wherein Z represents a C1-C6 chain hydrocarbon group and the like, R1 and R2 are identical to or different from each other and represent a hydrogen atom or a fluorine atom, and R3, R4, R5, R6 and R7 are identical to or different from each other and represent a C1-C6 chain hydrocarbon group and the like] to a plant or a soil, which has excellent control efficacies against plant diseases.
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- One-pot method for preparing O-alkyl hydroxylamine hydrochloride and N,O-dialkyl hydroxylamine hydrochloride
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The invention relates to the field of organic synthesis, in particular to a one-pot method for preparing O-alkyl hydroxylamine hydrochloride and N,O-dialkyl hydroxylamine hydrochloride. The method comprises the following steps: S1, acetylation: mixing hydroxylamine hydrochloride with water and methyl acetate, and dropwise adding a sodium hydroxide solution while stirring at room temperature to obtain an intermediate acetyl hydroxylamine; S2, alkylation: dropwise adding an alkylation reagent into the reaction kettle at normal temperature, and then heating the reactants for reaction; S3, hydrolysis and purification: after the reaction is qualified, adding concentrated sulfuric acid, performing heating hydrolysis, after the reaction is qualified, adding caustic soda flakes or liquid caustic soda to adjust the pH value to 12, carrying out atmospheric distillation and hydrochloric acid acidification, cooling the product for crystallization, and centrifuging and drying the crystal to obtaina final product. According to the invention, methyl acetate is used as an acetyl protective agent, and compared with ethyl acetate, methyl acetate has the advantages of good water solubility, small reaction steric hindrance, sufficient protection, few impurities, low price and cost and the like; therefore, the method has the advantages of high product purity, simple process operation, accessible raw materials, simple wastewater components and environment friendliness, and is suitable for industrial production.
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Paragraph 0032-0033
(2020/10/20)
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- Deoxyalkoxyamination of Alcohols for the Synthesis of N-Alkoxy-N-alkylbenzenesulfonamides
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A novel protocol for the deoxyalkoxyamination of alcohols has been developed, using N-alkoxybenzenesulfonimide (NOSI) as both a sulfonyl transfer reagent and an alkoxyamine source, accessing a diverse range of N-alkoxy-N-alkylbenzenesulfonamides with excellent isolated yields. This method is characterized by metal-free reaction, scalability, and waste-balance. Chiral substrates are converted with excellent levels of stereochemical inversion. NOSI could be generated in situ during the reaction as a stable reagent if a three-component one-pot reaction was designed. Exploiting this approach to run intramolecular reactions offered various N-protected isoxazolidines. In addition, valuable O-alkyl hydroxylamines (or isoxazolidines) were obtained through a neutral strategy of desulfonylation of the products.
- Sun, Qi-An,Lu, Ze-Hai,Pu, Xiao-Qiu,Hu, Hui-Lian,Zhang, Jia-heng,Yang, Xian-Jin
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supporting information
p. 3920 - 3927
(2018/07/31)
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- HIV INTEGRASE INHIBITORS
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The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
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- Studies on transannulation reactions across a nine-membered ring: The synthesis of natural product-like structures
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A series of diverse natural product-like structures have been synthesised by the use of a number of novel transannulation reactions across a cyclononene ring. Transannular cyclisations through oxygen functionality have generated a number of bicyclo[5.3.1]systems containing bridged cyclic ethers and bicyclo[5.2.2]lactones, as well as a tetrahydrofuran-containing bridged analogue of hexacyclinic acid. An unprecedented Bronsted acid mediated transannular cyclisation between proximal carbons generated bicyclo[4.3.0] nonanes which form the core of the pinguisane and austrodorane families of sesquiterpenoids. In all cases the key factor that determined the mode of reactivity was the conformation of the nine-membered ring and the distance between the reacting centres. The Royal Society of Chemistry 2011.
- Iqbal, Mudassar,Black, Richard J. G.,Winn, Joby,Reeder, Andrew T.,Blake, Alexander J.,Clarke, Paul A.
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experimental part
p. 5062 - 5078
(2011/08/21)
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- Discovery of [4-amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5- yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity
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The cyclin-dependent kinases (CDKs) and their cyclin partners are key regulators of the cell cycle. Since deregulation of CDKs is found with high frequency in many human cancer cells, pharmacological inhibition of CDKs with small molecules has the potential to provide an effective strategy for the treatment of cancer. The 2,4-diamino-5-ketopyrimidines 6 reported here represent a novel class of potent and ATP-competitive inhibitors that selectively target the cyclin-dependent kinase family. This diaminopyrimidine core with a substituted 4-piperidine moiety on the C2-amino position and 2-methoxybenzoyl at the C5 position has been identified as the critical structure responsible for the CDK inhibitory activity. Further optimization has led to a good number of analogues that show potent inhibitory activities against CDK1, CDK2, and CDK4 but are inactive against a large panel of serine/threonine and tyrosine kinases (Ki > 10 μM). As one of these representative analogues, compound 39 (R547) has the best CDK inhibitory activities (Ki = 0.001, 0.003, and 0.001 μM for CDK1, CDK2, and CDK4, respectively) and excellent in vitro cellular potency, inhibiting the growth of various human tumor cell lines including an HCT116 cell line (IC50 = 0.08 μM). An X-ray crystal structure of 39 bound to CDK2 has been determined in this study, revealing a binding mode that is consistent with our SAR. Compound 39 demonstrates significant in vivo efficacy in the HCT116 human colorectal tumor xenograft model in nude mice with up to 95% tumor growth inhibition. On the basis of its superior overall profile, 39 was chosen for further evaluation and has progressed into Phase I clinical trial for the treatment of cancer.
- Chu, Xin-Jie,DePinto, Wanda,Bartkovitz, David,So, Sung-Sau,Vu, Binh T.,Packman, Kathryn,Lukacs, Christine,Ding, Qingjie,Jiang, Nan,Wang, Ka,Goelzer, Petra,Yin, Xuefeng,Smith, Melissa A.,Higgins, Brian X.,Chen, Yingsi,Xiang, Qing,Moliterni, John,Kaplan, Gerald,Graves, Bradford,Lovey, Allen,Fotouhi, Nader
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p. 6549 - 6560
(2007/10/03)
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- METHOD FOR TREATING CHRONIC PAIN USING MEK INHIBITORS
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The invention features a method for treating chronic pain using a compound selected from formulae (I), (II)A, (I)B and (I)C.
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- Benzenesulfonamide derivatives and their use as MEK inhibitors
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Benzenesulfonamides of formula (I), in which W is OR1, NR2OR1, NRARB, NR2NRARB, or NR2(CH2)2-4NRARBand the other variables as defined in the claims, are inhibitors of MEK and are effective in the treatment of proliferative diseases, cancer, stroke, heart failure, xenograft rejection, arthritis, cystic fibrosis, hepatomegaly, cardiomegaly, Alzheimer's disease, complications of diabetes, septic shock, and viral infection.
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- Heteroaromate OSC inhibitors
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The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
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- Multicatalytic protease inhibitors
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Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: STR1 Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.
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- Process for preparing N,O-dialkylhydroxylamine, its salts or intermediates in their synthesis
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A process for preparing N,O-dialkylhydroxycarbamic acid ester which comprises reacting hydroxylamine or its salt with dihydrocarbyl carbonate in the presence of a basic compound to prepare hydroxycarbamic acid ester and subsequently alkylating this compound with an alkylating agent; a process for recovering N,O-dialkylhydroxycarbamic acid ester which comprises azeotropically distilling the ester with water from a solution containing the ester; a process for preparing N,O-dialkylhydroxylamine which comprises hydrolyzing N,O-dialkylhydroxycarbamic acid ester in an aqueous solution or a hydrous solvent in the presence of an alkali; a process for purifying N,O-dialkylhydroxylamine hydrochloride which comprises adding aldehyde or ketone to a solution of N,O-dialkylhydroxylamine hydrochloride containing O-alkylhydroxylamine hydrochloride as impurities to convert the O-alkylhydroxylamine hydrochloride into O-alkyl aldoxime or O-alkyl ketoxime and subsequently separating the N,O-dialkylhydroxylamine hydrochloride from the reaction system; and a process for separating N,O-dialkylhydroxylamine hydrochloride which comprises (i) adding benzene or alkylated benzene to an aqueous solution containing N,O-dialkylhydroxylamine hydrochloride, azeotropically removing water or a hydrochloride solution, and, subsequently (ii)adding alcohol thereto to obtain N,O-dialkylhydroxylamine hydrochloride in the form of crystal.
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- MULTICATALYTIC PROTEASE INHIBITORS
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Disclosed herein are inbibitors of the multicatalytic protease enzyme which are represented by the general formula: STR1 Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.
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- Method for preparation of sphingoid bases
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The present invention provides a series of non-toxic compounds which function to inhibit the activity of S-1-P aldolase in respect to its cleavage of S-1-P. These inhibitors are described by the compounds of formula I STR1 wherein R is a radical containing 1 to 15 carbon atoms, a halogen, or hydrocarbon, R' is an organic radical or hydrogen, and R" is --NH3+ or --NH--NH +, with the proviso that, when R is CH3 (CH)12 (CH=CH) and R' is hydrogen, R" is --NH--NH3+. A method for preparing such compounds, which may generally be described as 1-phosphate derivatives of compounds which include a 2-amino-1,3-alcohol radical is also disclosed.
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- 1-AMINOMETHYL-1,2,3,4-TETRAHYDRONAPHTHALENES
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Compounds of the formula STR1 and pharmaceutically acceptable salt thereof, wherein R 2 is selected from hydroxy and lower alkoxy, R 5 is lower alkyl, and R 11 and R 12 are independently selected from hydrogen, halo, hydroxy, methoxy, and lower alkyl, are selective . alpha.. sub.2 adrenergic receptor antagonists useful in the treatment of glaucoma.
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- 1-aminomethyl-1,2,3,4-tetrahydronaphthalenes
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The present invention provides compounds of the formula STR1 or a pharmaceutically acceptable salt thereof wherein R1 is selected from hydrogen, halo, lower alkyl, lower alkoxy, or thioalkoxy; and R2 is lower alkoxy; or R1 and R2 together form a methylenedioxy or ethylenedioxy ring; R3 and R4 are independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, (lower alkyl)amino, (lower alkylsulfonyl)amino, and halo; and R7 is selected from the group consisting of 2- or 3-thienyl, 2- or 3-furyl, and STR2 where R13 and R14 are independently selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower alkyl, lower alkoxy, lower alkylthio, methylenedioxy, or ethylenedioxy. The compounds of the present invention selectively inhibit α2 -adrenergic receptors as well as inhibit the uptake of biogenic amines and are thus useful in the treatment of certain cardiovascular and psychiatric disorders.
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- Iminium-Ion Formation and Deuterium Exchange by Acetone in the Presence of Pyrrolidine, Pyrazolidine, Isoxazolidine, and Their Acyclic Analogues
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Equilibrium constants for iminium-ion formation in the reaction of acetone in aqueous solution at 35 deg C with pyrazolidinium, isoxazolidinium, O,N-dimethylhydroxylammonium, and N,N'-dimethylhydrazinium ions were found to be 9.33, 8.96, 0.117, and 0.057 M-1, respectively.The kinetics of hydrolysis of the iminium ions were studied in every case except that of the N-isopropylidene-O,N-dimethylhydroxylammonium ion, whose hydrolysis is too fast to follow by the techniques used with the other iminium ions.The rate of hydrolysis of the N-isopropylidenepyrazolium ion is independent of the pH from about pH 3 to 6; it is hydrogen ion catalyzed at lower pHs and hydroxide ion catalyzed at higher pHs.The rate of hydrolysis of N-isopropylideneisoxazolidinium ions is pH independent from pH 0.5 to about 2, increases until about pH 4, remains pH independent until pH 6.5, and has become too fast to measure above pH 8.Both reactions are general base catalyzed in all the buffers studied.A mechanism is described to fit the kinetics of each of these reactions.The dedeuteration of acetone-d6 was studied in pyridine buffers in the presence of each of the four hydrazine and hydroxylamine derivatives and also in the presence of the dimethylammonium and pyrrolidinium ion (which was also studied in 3-dimethylaminopropionitrile buffers).All six of these secondary ammonium ions catalyze the dedeuteration by transforming the acetone-d6 to an iminium ion that is dedeuterated by pyridine more rapidly than the ketone is.The iminium-ion formation is a relatively rapid eqiuilibrium in all cases except that of pyrrolidinium ions, where the intermediate iminum ion loses deuterium and hydrolyzes at comparable rates, and possibly the case of dimethylammonium ions, where the amount of catalysis via iminium-ion formation is too small to reveal mechanistic details.The effect of structure on the efficiency of catalysis of dedeuteration via iminium-ion formation is discussed.
- Hine, Jack,Evangelista, Ramon A.
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p. 1649 - 1655
(2007/10/02)
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