- New strategy for detection of hydrogen peroxide based on bi-nucleophilic reaction
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Two novel fluorescent probes based on 7-hydroxy-4-methyl-coumarin, FAA-MC-OH (2-fluoro-4-nitro-phenylacetyl hydroxyl coumarin) and FBA-MC-OH (2-fluoro-4-nitro-benzoyl hydroxyl coumarin) are first synthesized, and spectral studies confirm that both the pro
- Liu, Xiang,Mao, Chenxin,Tian, Yafei,Wang, Bei,Wang, Shuoshuo
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- Preferred secondary structures as a possible driving force for macrocyclization
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The purpose of the work described in this paper was to explore links that may exist between conformational bias in macrocyclic products and the ease with which they are formed in solid phase S(N)Ar reactions. Solid phase synthesis of compounds 2 proceeds
- Reyes, Samuel,Pattarawarapan, Mookda,Roy, Sudipta,Burgess, Kevin
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- RAF INHIBITOR COMPOUNDS
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This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers.
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Page/Page column 36
(2013/09/26)
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- INHIBITORS OF JUN N-TERMINAL KINASE
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The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula (I): or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
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Page/Page column 99
(2010/08/18)
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- Benzo-fused heterocycles and carbocycles by intramolecular SNAr and tandem SN2-SNAr reactions
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(Chemical Equation Presented) Benzo-fused heterocyclic and carbocyclic systems have been synthesized by intramolecular SNAr and tandem SN2-SNAr reactions. Treatment of 3-(2-fluoro-5- nitrophenyl)-1-propanol with sodium hydride in N,N-dimethylformamide gave 6-nitrochroman in 80% yield by an intramolecular SNAr reaction. Treatment of 2-(3-bromopropyl)-1-fluoro-4-nitrobenzene with benzylamine in N,N-dimethylformamide gave 1-benzyl-6-nitrotetrahydroquinoline in 98% yield by a tandem SN2-SNAr reaction. Finally, in a similar process, reaction of this same bromide with dimethyl malonate under basic conditions gave 1,1-bis(methoxycarbonyl)-6-nitro-1,2,3,4-tetrahydronaphthalene in 80% yield. Further studies exploring ring size effects are also presented.
- Bunce, Richard A.,Nago, Takahiro,Sonobe, Nathan,Slaughter, LeGrande M.
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p. 551 - 557
(2008/09/18)
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- Oxazolidinones containing oxindoles as antibacterial agents
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The present invention relates to novel oxazolidinones derivatives of oxindoles of formula I, or a pharmaceutically acceptable salt thereof wherein Y1 is —CH— or —CF—; R1 is —C1-4alkyl, optionally substituted with a fluoro atom, or R1 is —C3-5cycloalkyl; and R2 is —H or —CH3. These compounds are useful as antibacterial agents.
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(2008/06/13)
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- Approaches to 1,1-disubstituted cinnolin-3-ylio oxides: Synthesis and reactivity of a new class of heterocyclic betaines
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The cinnolin-3-ylio oxides 6, a new class of heterocyclic aminimide, can be prepared by intramolecular cyclization of the N′,N′-disubstituted (2-fluorophenyl)acetohydrazides 5. Attempts to prepare these betaines by an alternative route, namely cyclization of the nitrenes expected from the thermal decomposition of (2-dialkylaminophenyl)acetyl azides 11, failed, Curtius rearrangement-derived compounds being the main products isolated from these processes. Hydrochlorides of the cinnolin-3-ylio oxides 6 undergo alkyl halide elimination to yield the 1-(ω-chloroalkyl)cinnolin-3-ols 19a,b or 1-methylcinnolin-3-ol 21. Oxidation of the latter to the 3-hydroxycinnolin-4-one 22, its methylation to the corresponding N1,O-23 and N1,N2-dimethyl 24 derivatives as well as the cyclization of 1-(5-chloropentyl)cinnolin-3-ol 19a to the diazepino[1,2-a]cinnolinone 20 are also reported.
- Aran, Vicente J.,Asensio, Juan L.,Molina, Jose,Munoz, Pilar,Ruiz, Jose R.,Stud, Manfred
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p. 2229 - 2235
(2007/10/03)
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