- PRODUCTION METHOD OF CYCLIC COMPOUND
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PROBLEM TO BE SOLVED: To provide an industrially simple production method of a cyclic compound. SOLUTION: A production method of a cyclic compound includes a step to obtain a reduced form (B) by reducing an unsaturated bond in a ring structure of an aromatic compound (A) by means of catalytic hydrogenation of the aromatic compound (A) or its salt using palladium carbon as a catalyst under a normal pressure, in which the aromatic compound (A) has one or more ring structures selected from a group consisting of a five membered-ring, a six membered-ring, and a condensed ring of the five membered-ring or the six membered-ring with another six membered-ring, a hetero atom can be included in the ring structure, and the aromatic compound (A) can have one or two side chains bonded to the ring structure and does not have any carbon-carbon triple bond in the side chain. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
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Paragraph 0057; 0059; 0062-0064
(2021/05/05)
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- Preparation method of 4 — acetoxypiperidine hydrochloride
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The invention discloses a preparation method of 4-acetoxypiperidine hydrochloride in the technical field of chemical synthesis. The preparation method comprises the following specific steps: S1, dissolving 8 to 10g of 4-piperidone hydrochloride into 30 to 40 ml of methanol; S2, performing rotary evaporation on filtrate to remove dichloromethane to obtain viscous liquid; S3, recrystallizing by using n-hexane to obtain 4-piperidinol; S4, separating an organic phase from an aqueous phase, extracting the aqueous phase by using ethyl acetate and combining the organic phase; S5, adding anhydrous sodium sulfate into the organic phase for drying and filtering to obtain white powder solid; S6, respectively adding acetic anhydride and a catalyst sulfamic acid and uniformly stirring; S7, recrystallizing by using ethanol to obtain a white 4-acetoxypiperidine hydrochloride solid. The preparation method of the 4-acetoxypiperidine hydrochloride, disclosed by the invention, has the advantages of simple preparation process, no special requirements on equipment and no danger in the preparation process; in addition, a prepared 4-acetoxypiperidine hydrochloride finished product has the advantages of high yield, high purity and suitability for factory large-scale synthesis.
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Paragraph 0019-0024
(2021/11/27)
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- Method for regulating and controlling catalytic hydrogenation reaction of pyridine derivative with redox potential
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The invention discloses a method for regulating and controlling catalytic hydrogenation reactions of a pyridine derivative with redox potential. On the basis of data such as redox potential (ORP) andcatalytic hydrogenation reaction process of the pyridine derivative in different medium systems, a scheme that the catalytic hydrogenation reaction of the pyridine derivative is promoted by improvingpyridine derivative ORP with an acid water solution is proposed. As the catalytic hydrogenation reactions of the pyridine derivative are instructed with ORP data, the testing period is shortened, meanwhile, by adopting the process, the pressure of hydrogenation reactions can be reduced, a piperidine product has the advantages of being high in purity, convenient in aftertreatment, and the like, andthus great instruction significances can be achieved for industrial development of the pyridine derivative.
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Paragraph 0036-0043
(2019/05/08)
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- Boiling water-catalyzed neutral and selective N-Boc deprotection
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A general protocol for removing Boc groups from various types of nitrogen is reported and a preliminary investigation of the reaction mechanism indicates that water acts as a dual acid/base catalyst at elevated temperature. The Royal Society of Chemistry 2009.
- Wang, Jia,Liang, Yan-Liang,Qu, Jin
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supporting information; experimental part
p. 5144 - 5146
(2009/12/08)
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- Novel dimeric aryldiketo containing inhibitors of HIV-1 integrase: Effects of the phenyl substituent and the linker orientation
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Aryl diketoacids (ADK) and their bioisosteres are among the most promising HIV-1 integrase (IN) inhibitors. Previously, we designed a series of ADK dimers as a new class of IN inhibitors that were hypothesized to target two divalent metal ions on the active site of IN. Herein we present a further structure-activity relationship (SAR) study with respect to the substituent effect of the ADK and the dimerization with conformationally constrained linkers such as piperazine, 4-amino-piperidine, piperidin-4-ol, and trans-cyclohexan-1,4-diamine. The substituents on the phenyl ring as well as the spatial orientation of the two diketo units were observed to play important roles in the IN inhibitory potency. The hydrophobic group was an optimal substitution at the 3-position of the aryl ring. The piperazine and 4-amino-piperidine linkers brought about the most potent analogs among the hydrophobic group or halogen substituted ADK dimers. The docking studies suggested that the bulky hydrophobic substitution at 3-phenyl ring and the linker of 4-amino-piperidine were beneficial for adopting an active conformation to achieve strong interactions with the active site Mg2+ and the key residue E152 within the catalytic core domain. This study is a significant extension of our previous report on the dimeric ADK-containing IN inhibitors, providing a new promising template for further lead optimization.
- Zeng, Li-Fan,Jiang, Xiao-Hua,Sanchez, Tino,Zhang, Hu-Shan,Dayam, Raveendra,Neamati, Nouri,Long, Ya-Qiu
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p. 7777 - 7787
(2008/12/23)
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- Selectivity in the electrochemical deprotection of cinnamyl groups from oxygen and nitrogen functionalities: Carbonates versus carbamates
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Several cinnamyloxy carbamates and carbonates were subjected to electrochemical reduction, and the reductive fate of the cinnamyl group was investigated. Complete selectivity was observed in the removal of the cinnamyl group from oxygen versus nitrogen.
- Canka?, Petr,Dubas, Diane,Banfield, Scott C.,Chahma, M'hamed,Hudlicky, Tomas
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p. 6851 - 6854
(2007/10/03)
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- Chemoselective deprotection of allylic amines catalyzed by Grubbs' carbene
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A commercially available ruthenium complex (first generation Grubbs' carbene) was used for the catalytic deprotection of allylic amines (secondary as well as tertiary), by using for the first time reagents different from palladium catalysts. Interestingly, the catalytic system directs the reaction toward the selective deprotection of allylamines in the presence of allylic ethers.
- Alcaide, Benito,Almendros, Pedro,Alonso, Jose M.,Luna, Amparo
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p. 668 - 672
(2007/10/03)
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- Methods and compounds for treating proliferative diseases
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The compounds disclosed herein are indolocarbazoles of Formula (I), which are potent CDK4 inhibitors, and are useful in the treatment of cell proliferative disorders, including cancer. Formula (I).
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Anti-HCV nucleoside derivatives
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The present invention comprises novel and known purine and pyrimidine nucleoside derivatives which have been discovered to be active against hepatitis C virus (HCV). The use of these derivatives for the treatment of HCV infection is claimed as are the novel nucleoside derivatives disclosed herein.
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- Samarium diiodide-induced couplings of carbonyl compounds with methoxyallene leading to 4-hydroxy 1-enol ethers
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(Matrix presented) A surprising samarium diiodide-induced coupling reaction of carbonyl compounds with methoxyallene provided 4-hydroxy 1-enol ethers, which are versatile synthetic building blocks. In this coupling reaction, methoxyallene serves as an acrolein equivalent, which cannot directly be employed.
- Hoelemann, Alexandra,Reissig, Hans-Ulrich
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p. 1463 - 1466
(2007/10/03)
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- Benzothiazole derivatives with activity as adenosine receptor ligands
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The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.
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- Noble metal Raney catalysts and preparation of hydrogenated compounds therewith
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Noble metal, particularly ruthenium, Raney catalysts having the property of catalyzing the hydrogenation of (1) aromaticity-exhibiting ring portions of organic compounds, (2) carboxylic acids and their ester portions (carbonyl ester groups), (3) ring portions and carboxylic acid or their ester groups in compounds having such ring portions and carboxylic acid or their ester portions, and (4) ring portions and nitrile groups of aromatic nitrile compounds and methods for the preparation of corresponding hydrogenated compounds. The methods allow preparation of hydrogenated compounds having hydrogenated aromatic ring portions, hydrogenated carbonyl ester groups, hydrogenated aromatic ring and carbonyl ester groups, or hydrogenated aromatic rings and nitrile groups under milder hydrogen pressure and temperature conditions than the conventional catalysts.
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- 8-chloro-1-cyclopropyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid and alkyl esters thereof
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The invention is related to 7-amino-1-cyclopropyl-6,8-dihalogeno-1,4-dihydro-4-oxo-3-quinoline-carboxylic acids of the formula (I) STR1 in which X1, X2, R1 and R2 have the meaning as pointed out in the following specification. Moreover, the invention is related to a process for the production of the compounds of formula (I) and to antibacterial agents containing them.
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- 2,3,4,5-tetrahalogenobenzene derivatives
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2,3,4,5-trihalogenobenzene derivatives of the formula STR1 in which R is --COOH, --COCl, --COF, --CN, --CONH2, --CH2 OH, --CH2 Cl, --CHCl2, --CCl3 or --CHO, R1 is H, Cl or F, and R2 is Cl or F, it only being possible for R1 or R2 to be F, and processes for their preparation starting from benzonitriles reacted with potassium fluoride. The novel compounds are intermediates for antibacterials such as quinolone carboxylic acids.
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- Process for the preparation of N-allyl-piperidine derivatives
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A process is described for the preparation of N-allyl-2,2,6,6-tetraalkyl-piperidine derivatives which involves reaction of the corresponding 2,2,6,6-tetraalkyl-piperidine with an allylic carbonate in the presence of palladium catalysts. The products which are thus obtained are useful as polymer stabilizers and chemical intermediates.
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- C20 Through C26 amino steroids
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Disclosed are Δ9 (11)-steroids (VI) and amino substituted steroids of formula (XI) which contain an amino group attached to the terminal carbon atom of the C17-side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ16 (11)-steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ17 (20)-steroids (Va and Vb) and Δ9 (11)-steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
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- PROTECTION OF PRIMARY AND SECONDARY AMINES IN THE HYDROBORATION REACTION
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Trimethylsilyl groups are efficient to protect the N-H bonds of olefinic amines in the hydroboration reaction with BMS; deprotection is easily run with methanol and affords aminoorganoboranes which can be used without any oxydation.
- Dicko, A.,Montury, M.,Baboulene, M.
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p. 6041 - 6044
(2007/10/02)
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- Process for preparation of N-allyl-piperidine derivatives
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A process is described for the preparation of N-allyl-2,2,6,6-tetraalkyl-piperidine derivatives which involves reaction of the corresponding 2,2,6,6-tetraalkyl-piperidine with an allylic carbonate in the presence of palladium catalysts. The products which are thus obtained are useful as polymer stabilizers and chemical intermediates.
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- Anthelmintic 5(6)-benzene ring substituted benzimidazole-2-carbamates
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Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: STR1 where R is a lower alkyl group having 1 to 4 carbon atoms; STR2 is a 5, 6, 7 or 8 membered heterocyclic ring containing 1 to 2 hetero atoms; the STR3 substitution being at the 5(6)-position; and the pharmaceutically acceptable salts thereof. The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.
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- Fluorodehydroxylation of serine
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Organic compounds containing one or more alcoholic hydroxyl groups are transformed into fluorine compounds by reacting them with sulfur tetrafluoride in liquid hydrogen fluoride solution, at temperatures between around -80° C. and +20° C. The method can be descriptively termed "fluorodehydroxylation", because it represents the reaction:
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- 3,6-Bis-(heterocyclic aminoacyl-amino)-acridines and salts thereof
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Compounds of the formula STR1 wherein R1 is hydrogen or methyl, R2 and R3, together with each other and the nitrogen atom to which they are attached, form a saturated or unsaturated heterocyclic ring system which may optionally contain one or more additional heteroatoms, and A is lower alkylene or aryl-lower alkylene, and nontoxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as inducers of the formation of interferon.
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