- A process for preparing 4, 4 - pyran dicarboxylic acid diethyl ester derivative method
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The invention relates to a method for preparing 4,4-pyran diethyl dicarboxylate and a derivative thereof. According to the invention, diethyl malonate and substituted dichloroethyl ether are adopted as raw materials; cuprous iodide is used for catalyzing; one or a mixture of compounds selected from potassium tert-butoxide, sodium tert-butoxide and sodium tert-pentoxide is adopted as an alkali, and a reaction is carried out; when the reaction is finished, a solvent is removed by reduced-pressure distillation; and reduced-pressure distillation is continued, such that 4,4-pyran diethyl dicarboxylate or the derivative thereof are obtained. The method provided by the invention has never been reported before. The raw materials are easy to obtain, the reaction method is simple and feasible, and the reaction time is short. The method has high application and market values.
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Paragraph 0019-0030
(2017/07/31)
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- 2-OXO-2- (2-PHENYL-5,6,7,8-TETRAHYDRO-INDOLIZIN-3-YL) -ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ANTIFUNGAL AGENTS
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The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
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Page/Page column 14
(2011/02/15)
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- 2- [ (2-SUBSTITUTED) -IND0LIZIN-3-YL] -2-OXO-ACETAMIDE DERIVATIVES AS ANTIFUNGAL AGENTS
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The invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof wherein: Rl, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. These compounds are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
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Page/Page column 110
(2008/12/05)
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- Pharmaceutical compositions and methods for effecting dopamine release
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Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a 1-aza-2-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-2-(3-pyridyl)bicyclo[2.2.2]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.1]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.2]nonane, a 1-aza-7-(3-pyridyl) bicyclo[2.2.1]heptane, a 1-aza-3-(3-pyridyl)bicyclo[3.2.2]nonane, or a 1-aza-7-(3-pyridyl)bicyclo[3.2.2]nonane. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.
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- Processes for preparing 3-Arylsulfur hydroxamic acids
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This invention provides processes for the preparation of a compound of Formula I: Y—C(═O—C(R1)(R2)—CH2—S(O)nR3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R1is hydrogen or lower alkyl; R2is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1and R2together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R3is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.
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- 112. Novel heterospirocyclic 3-amino-2H-azirines as synthons for heterocyclic α-amino acids)
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The heterospirocyclic N-methyl-N-phenyl-2H-azirin-3-amines (3-(N- methyl-N-phenylamino)-2H-azirines) 1a-d with a tetrahydro-2H-pyran, tetrahydro-2H-thiopyran, and a N-protected piperidine ring respectively, were synthesized from the corresponding heterocyclic 4-carboxamides 2 by consecutive treatment with lithium diisopropylamide (LDA), diphenyl phosphorochloridate (DPPCl), and sodium azide (Scheme 4). The reaction of these aminoazirines with thiobenzoic acid in CH2Cl2 at room temperature gave the thiocarbamoyl-substituted benzamides 13a-d in high yield. The azirines 1a-d were used as synthons for heterocyclic α-amino acids in the preparation of tripeptides of the type Z-Aib-Xaa-Aib-N(Ph)Me (18) by following the protocol of the 'azirine/ox-azolone method': treatment of Z- Aib with 1 to give the dipeptide amide 15, followed by selective hydrolysis to the corresponding acid 16 and coupling with the 2,2-dimethyl-2H-azirin-3- amine 17 gave 18, again in high yield (Scheme 5). With some selected examples of 18, the selective deprotection of the amino and the carboxy group, respectively, was demonstrated (Scheme 6). The solid-state conformations of the protected tripeptides 18a-d, as well as that of the corresponding carbocyclic analogue 18e, were determined by X-ray crystallography (Figs. 1- 3 and Tables 1-3). All five tripeprides adopt a β-turn conformation of type III or III. The solvent dependence of the chemical shifts of the NH resonances (Fig. 6) suggests that there is an intramolecular H-bond between H-N(4) and O(11) in all cases, which is an indication that a relatively rigid β-turn structure also persists in solution. Surprisingly, the tripeptide acid 20a shows no intramolecular H-bond in the crystalline state (Fig. 7); O(11) is involved in an intermolecular H-bond with the OH group of the carboxy function.
- Straessler, Christoph,Linden, Anthony,Heimgartner, Heinz
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p. 1528 - 1551
(2007/10/03)
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- Depolarizing skeletal muscle relaxants
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Compounds such as [5-chloronicotine, 5-fluoronornicotine, anabaseine, 5-fluoroanabaseine, 2-acetoxymethylquinuclidine or]2-(3-pyridyl)-quinuclidine are useful as locally acting and highly selective muscle relaxants. Each compound, when administered intravenously, acts to bind to musculoskeletal nicotinic receptor sites in a reversible manner causing transient depolarization, and hence provides for reversible muscle relaxation to a patient during anesthesia.
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- SYNTHESIS OF OXOSULFONIUM SALTS BY THE OXIDATION OF SULFONIUM SALTS
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A general synthetic method for oxosulfonium salts by oxidation of sulfonium salts with sodium perbenzoate (or sodium m-chloroperbenzoate) was developed.In case of the oxidation of aryldimethylsulfonium salts, the corresponding oxosulfonium salts (1e-h) were obtained in 64-91percent yields.Diphenylmethylsulfonium and triphenylsulfonium salts were also oxidized with sodium perbenzoate to afford the corresponding oxosulfonium salts (1i and 1j) in 75 and 58percent yields, respectively.Trialkylsulfonium salts such as trimethylsulfonium, dimethyloctylsulfonium, S-methylthiolanium, and S-methyl(pentamethylene)sulfonium salts, were also oxidized to the corresponding oxosulfonium salts (1a-d) in good yields.To clarify the reaction mechanisms, the oxidation of bicycloheptane-1-sulfonium salt (5) was investigated and found to afford oxosulfonium salt (6) in 50percent yield.A reaction mechanism involving nucleophilic attack by perbenzoate anion on the cationic sulfur atom of sulfonium salt and giving an S-O sulfurane intermediate is proposed.
- Mori, Mitsuo,Takeuchi, Hiroyuki,Minato, Hiroshi,Kobayashi, Michio,Yoshida, Masato,et al.
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p. 157 - 164
(2007/10/02)
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- Cationic complexes of technetium-99m
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The invention concerns cationic complexes of Technetium-99m with bidentate ligands (L), including complexes having the formulae [Tc(NO) X L2 ]+ and [Tc L3 ]+, which are of interest as heart imaging agents. The ligands are characterized by having the formula Y2 QZQY2, where each Q is phosphorus or arsenic, Z is a 2 or 3 carbon atom linking group, and at least one of the groups Y and Z includes at least one --COC--ether group.
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