201406-78-2Relevant articles and documents
Tricyclic dihydroimidazopyrimidinone derivative, and preparation method, pharmaceutical composition and application thereof
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Paragraph 0271-0274, (2021/05/12)
The invention provides a compound as shown in a general formula (I), cis-trans isomers, enantiomers, diastereoisomers, racemes, solvates, hydrates or pharmaceutically acceptable salts or prodrugs of the compound, a preparation method of the compound, a pharmaceutical composition containing the compound and an application of the compound as aLp-PLA2 inhibitor, wherein R1, R2, Rx, Ra, Q, U, X, Y, m, n and A are defined in the specification.
USE OF AMINOINDANE COMPOUNDS IN TREATING OVERACTIVE BLADDER AND INTERSTITIAL CYSTITIS
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, (2014/03/22)
The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient.
Aminoindane Compounds and Use Thereof in Treating Pain
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, (2012/09/05)
The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV 1 receptor activator. In one embodiment, the TRPV 1 receptor activator is lidocaine.
Water-compatible iminium activation: Organocatalytic Michael reactions of carbon-centered nucleophiles with enals
Palomo, Claudio,Landa, Aitor,Mielgo, Antonia,Oiarbide, Mikel,Puente, Angel,Vera, Silvia
, p. 8431 - 8435 (2008/09/19)
(Chemical Equation Presented) A pool of water-compatible catalysts, namely the chiral prolinol-based catalysts 1, has been developed for highly enantioselective C-C bond-forming Michael reactions in water (see scheme). The synthesis of (S)-Rolipram, a type IV phosphodiesterase inhibitor, was also demonstrated.
A mild and efficient cyanosilylation of ketones catalyzed by a Lewis acid-Lewis base bifunctional catalyst
Shen, Yongcun,Feng, Xiaoming,Li, Yan,Zhang, Guolin,Jiang, Yaozhong
, p. 5667 - 5675 (2007/10/03)
A new family of bifunctional catalysts (N-oxides-Ti(OiPr)4 (2:1)) containing a Lewis acid and a Lewis base was developed and applied to the catalytic cyanosilylation of ketones. Utilizing rac((1R,2S) and (1S,2R))-1-(2′-pyridylmethyl)-2-diphenylhydroxymethylpyrrolidine N-oxide-titanium (2:1) complex and N-benzyl-diethanolamine N-oxide-titanium (2:1) complex as catalysts, the cyanosilylation products were obtained in 42-97% yield. Based on experimental phenomena and kinetic studies, a catalytic cycle was proposed to explain the remarkable activities of these catalysts. Investigations indicated that rac((1R,2S) and (1S,2R))-1-(2′-pyridylmethyl)-2-diphenylhydroxymethylpyrrolidine N-oxide-titanium (2:1) complex and N-benzyl-diethanolamine N-oxide-titanium (2:1) complex should promote the reaction via a dual activation of the ketone by the titanium and TMSCN by the N-oxide.
Use of polymer supported reagents for clean multi-step organic synthesis: Preparation of amines and amine derivatives from alcohols for use in compound library generation
Ley, Steven V.,Bolli, Martin H.,Hinzen, Berthold,Gervois, Anne-Geraldine,Hall, Beverley J.
, p. 2239 - 2241 (2007/10/03)
The automated sequential application of polymer supported perruthenate (PSP) and polymer supported cyanoborohydride (PSCBH) in an oxidation-reductive amination procedure allowed the efficient transformation of simple alcohols into more complex amines which can be further derivatised by the use of polymer bound amino sulfonylpyridinium chlorides.
Catalytic epoxidation of unfunctionalized alkenes by dinuclear nickel(II) complexes
Rispens, Minze T.,Gelling, Onko Jan,De Vries, Andre H.M.,Meetsma, Auke,Van Bolhuis, Fre,Feringa, Ben L.
, p. 3521 - 3546 (2007/10/03)
The synthesis, crystal and molecular structure and catalytic activity in epoxidation reactions of new dinuclear nickel(II)-complexes, octahedral μ-diacetato-μ-[2,6-bis[N-2-2'-pyridylethyl)formimidoyl]phenolato]bis nickel(II)·perchlorate·methanol (6) and square planar (μ-hydroxo-μ-[2,6-bis[N-((S)-1-benzyl-2-yl-pyrrolidine)formimidoyl]p henolato]bisnickel(II)·bisperchlorate (7), are described. For the preparation of 7 a new 5-step route for homochiral bisamine (S)-benzyl-2-aminomethyl-pyrrolidine (19) was developed starting from (S)-proline. Epoxidation of unfunctionalized alkenes with sodium hypochlorite and tert-butyl hydroperoxide as terminal oxidants was effectively catalyzed with bisnickel(II)-complexes 6 and 7, and a turnover of 165 was reached using trans-β-methylstyrene (34). The epoxidations probably proceed via a radical intermediate (such as OCl·) and no enantioselectivity is obtained under phase transfer conditions. In epoxidation reactions employing tert-butyl hydroperoxide as terminal oxidant a turnover of 43 was obtained with trans-stilbene (30) as substrate. Unexpectedly in the case of styrene (29) 1,2-bis-(tert-butylperoxy)ethylbenzene (59) was isolated as the major product.
