16153-63-2Relevant academic research and scientific papers
Exploring Homogeneous Conditions for Mild Buchwald-Hartwig Amination in Batch and Flow
Kashani, Saeed K.,Jessiman, Jacob E.,Newman, Stephen G.
, p. 1948 - 1954 (2020)
Cross-couplings are among the most frequently used reactions in complex molecule synthesis. However, the requirement of stoichiometric base can cause challenges. Harsh, insoluble inorganic bases can lead to poor tolerance of sensitive functional groups, scale-up issues, and difficult adaptation to continuous flow platforms. Herein, we describe the use of high throughput experimentation to identify a number of conditions that enable Buchwald-Hartwig reactions to be carried out using readily available ligands (e.g., XantPhos) with DBU as a soluble, functional-group-tolerant, homogeneous base. Application of this system to diverse aminations in batch and flow are demonstrated, as is the translation of this technique to performing continuous Mizoroki-Heck and Sonogashira coupling reactions.
AMINONAPTHOQUINONE COMPOUNDS AND PHARMACEUTICAL COMPOSITION FOR BLOCKING UBIQUITINATION-PROTEASOME SYSTEM IN DISEASES
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Paragraph 00201, (2017/02/09)
The invention relates to new compounds with low cytotoxicity for blocking the ubiquitination- proteasome system in diseases. Accordingly, these compounds can be used in treatment of disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders, autoimmune disorders and metabolic disorders.
Effective nitration of anilides and acrylamides by tert-butyl nitrite
Ji, Yi-Fei,Yan, Hong,Jiang, Qi-Bai
, p. 2051 - 2060 (2015/03/18)
Nitro compounds are important intermediates in synthetic organic chemistry and the chemical industry. Herein, the efficient copper-catalyzed [10% Cu(NO3)2·3H2O] nitration of anilides was developed by using TBN (tert-butyl nitrite) as a nitrating reagent to give the corresponding nitro-substituted aromatic products in good to excellent yields. The use of TBN also led to the selective nitration of acrylamides at room temperature to afford only the (E) isomer of the nitration product. A series of anilides and acrylamides with a broad array of functional groups were well-tolerated by this procedure. This synthetic method has many advantages, which include inexpensive starting materials, mild reaction conditions, a fast reaction rate, and high yields. A mechanistic investigation indicates that a nitro radical, which is generated from the thermal homolysis of TBN, is involved in the two nitration processes. The efficient nitration of both anilides and acrylamides was achieved by using TBN (tert-butyl nitrite) as a metal-free nitrating reagent. This synthetic method has many advantages such as mild reaction conditions, a fast reaction rate, good to excellent yields, and a broad substrate scope. Our investigation indicates that a nitro radical is involved in the reaction mechanism.
Pyridinium cationic-dimer antimalarials, unlike chloroquine, act selectively between the schizont stage and the ring stage of Plasmodium falciparum
Yoshikawa, Mai,Motoshima, Kazunori,Fujimoto, Kanji,Tai, Akihiro,Kakuta, Hiroki,Sasaki, Kenji
, p. 6027 - 6033 (2008/12/22)
Malaria is a leading cause of death in developing countries, and the emergence of strains resistant to the main therapeutic agent, chloroquine, has become a serious problem. We have developed cationic-dimer type antimalarials, MAP-610 and PMAP-H10, which
