- Transition-metal-free mono- or dinitration of protected anilines
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An amide-assisted arene nitration is presented, and both mono- and dinitration of protected anilines could be effected by using NaNO2 and NaNO3 as the mono- and bisnitrating agents, respectively. This divergent synthesis is transition-metal- and acid-free, and features a broad substrate scope, low cost, and ortho–para selectivity.
- Dai, Enrui,Dong, Ying,Dong, Yongrui,Kong, Rui,Liang, Deqiang,Liu, Guangzhang,Ma, Yinhai,Wu, Qiong
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- PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
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Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
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Page/Page column 87
(2012/02/01)
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- Synthesis of mono-substituted derivatives of 6-aminoquinoline
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Several 6-aminoquinoline derivatives, which could be used in drug design, have been synthesized. The reaction conditions were comparatively studied, and the p-chloroaniline was used as optimum oxidant in Skraup-Doebner-Von Miller reaction. The nitro group was reduced effectively by SnCl2 with no halo-removed occurred.
- Lan, Tian,Yuan, Xian Xia,Yu, Jiang Hong,Jia, Chao,Wang, Yu Shi,Zhang, Hui Juan,Ma, Zi Feng,Ye, Wei Dong
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p. 253 - 255
(2012/01/04)
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- BENZIMIDAZOLECARBOXAMIDES AS INHIBITORS OF FAK
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This invention relates to benzimadolecarboxamides of formula (I) which are inhibitors of focal adhesion kinase, and as such are useful for treating proliferative diseases
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Page/Page column 100
(2010/11/17)
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- Spectral tuning of azobenzene photoswitches for biological applications
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Longer switching wavelengths and good photochemical yields and stabilities of the cis isomers in reducing aqueous environments are achieved by introducing 2,2 -aminoalkyl substituents into 4,4 - diamido-substituted azobenzenes. The products are thus suita
- Sadovski, Oleg,Beharry, Andrew A.,Zhang, Fuzhong,Woolley, G. Andrew
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scheme or table
p. 1484 - 1486
(2009/07/25)
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- Nitric acid in the presence of P2O5 supported on silica gel - A useful reagent for nitration of aromatic compounds under solvent-free conditions
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A variety of aromatic compounds are nitrated to parent nitro aromatic compounds under solvent-free conditions using 65% nitric acid in the presence of P2O5 supported on silica gel is described. This methodology is useful for nitration of activated and deactivated aromatic rings.
- Hajipour, Abdol Reza,Ruoho, Arnold E.
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p. 8307 - 8310
(2007/10/03)
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- A fast and mild method for nitration of aromatic rings
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The use of benzyltriphenylphosphonium nitrate (PhCH2Ph 3P+NO3-) (BTPPN) as a useful reagent for nitration aromatic compounds in the presence of methanesulfonic anhydride under solvent-free conditions is described. This methodology is useful for nitration of activated aromatic rings.
- Hajipour, Abdol R.,Ruoho, Arnold E.
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p. 221 - 226
(2007/10/03)
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- Ozone-mediated Reaction of Anilides and Phenyl Esters with Nitrogen Dioxide: Enhanced Ortho-reactivity and Mechanistic Implications
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In the presence of ozone, anilides 1 can be nitrated rapidly with nitrogen dioxide in chloroform at 0 deg C to give a high proportion of ortho-nitro derivatives (ortho:para = 1.2-4.4) in good yields.The phenyl esters 15 can be similarly nitrated on the aromatic ring without significant cleavage of the ester bond, giving a mixture of isomeric nitro derivatives in which the ortho-isomer predominantes (ortho:para = 1.1-1.5).The oridin of the enhanced ortho reactivity is discussed in terms of an electron-transfer process involving the nitrogen trioxide as initial electrophile.
- Suzuki, Hitomi,Tatsumi, Atsuo,Ishibashi, Taro,Mori, Tadashi
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p. 339 - 344
(2007/10/02)
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- Anthelmintically active benzenepropanamide derivatives
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This invention is directed to a method for treating helminthiasis in an animal which method comprises administering to an animal in need thereof an anthelmintically effective amount of a compound of the Formula (I): STR1 wherein Z is oxygen or sulfur;R 1 is hydrogen or lower alkyl; andR 2, R 3, R 4 and R 5 are independently hydrogen, halo, lower haloalkyl, lower alkoxy, lower haloalkoxy, nitro, cyano, halophenoxy, haloalkylphenoxy, thiocyano or isothiocyano, provided that R 2 and R 3 cannot simultaneously be hydrogen and that R 4 and R 5 cannot simultaneously be hydrogen; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions formulated therewith. This invention is also directed to novel anthelmintically active benzenepropanamides of Formula (I) wherein Z is oxygen.
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- Ortho-Selective Nitration of Acetanilides with Nitrogen Dioxide in the Presence of Ozone
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In the presence of ozone, nitrogen dioxide rapidly reacts with acetanilides ortho-selectively at low temperatures, giving a high proportion of ortho-nitro derivatives in good yields.
- Suzuki, Hitomi,Ishibashi, Taro,Murashima, Takashi,Tsukamoto, Kenkichi
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p. 6591 - 6594
(2007/10/02)
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