861931-75-1Relevant academic research and scientific papers
Synthesis method and intermediate for 2-bromo-5-fluoro-4-nitroaniline
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, (2020/01/12)
The invention discloses a synthesis method and an intermediate for 2-bromo-5-fluoro-4-nitroaniline. The synthesis method for 2-bromo-5-fluoro-4-nitroaniline comprises the step of carrying out a nitration reaction on 2-bromo-5-fluoroaniline and a nitration reagent to generate the 2-bromo-5-fluoro-4-nitroaniline, or comprises the following steps: reacting the 2-bromo-5-fluoroaniline with an amino protection reagent to obtain amino-protected 2-bromo-5-fluoroaniline, then carrying out the nitration reaction on the amino-protected 2-bromo-5-fluoroaniline and the nitration reagent to generate a nitration product that is the intermediate, and finally, removing the amino protection group from the nitration product to obtain the 2-bromo-5-fluoro-4-nitroaniline. The synthesis method has the advantages of high reaction yield, high product purity and easily available raw materials.
Homogenous suspension of immunopotentiating compounds and uses thereof
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Page/Page column 66, (2016/09/12)
The present invention generally relates to homogeneous suspensions of small molecule immune potentiators (SMIPs) that are capable of stimulating or modulating an immune response in a subject in need thereof. The homogeneous suspensions may be used in combinations with various antigens or adjuvants for vaccine therapies.
Synthesis of new indole-based bisphosphonates and evaluation of their chelating ability in PE/CA-PJ15 cells
Palmerini, Carlo A.,Tartacca, Francesco,Mazzoni, Michela,Granieri, Letizia,Goracci, Laura,Scrascia, Angela,Lepri, Susan
, p. 403 - 412 (2015/09/01)
Bisphosphonates are the most important class of antiresorptive agents used against osteoclast-mediated bone loss, and, more recently, in oncology. These compounds have high affinity for calcium ions (Ca2+) and therefore target bone mineral, whe
Development of a Br?nsted acid-promoted arene-ynamide cyclization toward the total syntheses of marinoquinolines A and C and aplidiopsamine A
Yamaoka, Yousuke,Yoshida, Takahiro,Shinozaki, Makiko,Yamada, Ken-Ichi,Takasu, Kiyosei
, p. 957 - 964 (2015/03/05)
(Chemical Equation Presented) A Br?nsted acid-promoted arene-ynamide cyclization has been developed to construct the 3H-pyrrolo[2,3-c]quinolines. This reaction consists of the generation of a highly reactive keteniminium intermediate from arene-ynamide activated by a Br?nsted acid and electrophilic aromatic substitution reaction to give arene-fused quinolines in high yields. This methodology enabled facile access to marinoquinolines A and C and aplidiopsamine A.
Palladium-catalyzed annulation of haloanilines and halobenzamides using norbornadiene as an acetylene synthon: A route to functionalized indolines, isoquinolinones, and indoles
Thansandote, Praew,Hulcoop, David G.,Langer, Michael,Lautens, Mark
supporting information; experimental part, p. 1673 - 1678 (2009/07/17)
A general procedure for the palladium-catalyzed annulation of substituted haloanilines with norbornadiene gives functionalized indolines in 51-98% yield. These indolines can be rapidly converted to benzenoid- substituted indoles and tricyclic indolines. Extension to the use of substituted halobenzamides gives functionalized isoquinolinones in up to 86% yield.
COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS
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Page/Page column 172, (2009/10/22)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors, including TLR7 and TLR8. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine (formula I) wherein: X3 is N; X4 is N Or CR3; X5 is -CR4=CR5.
Nucleus- and side-chain fluorinated 3-substituted indoles by a suitable combination of organometallic and radical chemistry
Bellezza, Francesca,Cipiciani, Antonio,Ruzziconi, Renzo,Spizzichino, Sara
, p. 97 - 107 (2008/12/20)
Regioselectively fluoro-, trifluoromethyl- and trifluoromethoxy-substituted 3-methyleneindolines have been prepared using a four-step procedure involving metalation/bromination of fluorinated Boc-protected anilines, N-propargylation of the resulting o-bro
SELECTIVE ESTROGEN RECEPTOR MODULATORS FOR THE TREATMENT OF VASOMOTOR SYMPTOMS
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Page/Page column 109-110, (2008/06/13)
The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
