1362296-02-3Relevant academic research and scientific papers
Hexafluoroisopropanol-Mediated Redox-Neutral α-C(sp3)-H Functionalization of Cyclic Amines via Hydride Transfer
Shen, Yao-Bin,Wang, Lin-Xuan,Sun, Yun-Ming,Dong, Feng-Ying,Yu, Liping,Liu, Qing,Xiao, Jian
, p. 1915 - 1926 (2020/02/04)
Hexafluoroisopropanol has been demonstrated as the versatile promoter for redox-neutral α-C(sp3)-H functionalization of cyclic amines via the cascade [1,5]-hydride transfer/cyclization strategy. A wide range of cyclic amines are functionalized
Redox-Neutral Cascade Dearomatization of Indoles via Hydride Transfer: Divergent Synthesis of Tetrahydroquinoline-Fused Spiroindolenines
Shen, Yao-Bin,Li, Long-Fei,Xiao, Ming-Yan,Yang, Jian-Ming,Liu, Qing,Xiao, Jian
, p. 13935 - 13947 (2019/11/11)
The redox-neutral cascade dearomatization of indoles with o-aminobenzaldehydes has been realized via the hydride transfer strategy, achieving the condition- A nd substrate-controlled divergent synthesis of tetrahydroquinoline-fused spiroindolenines. The integration of hydride transfer-involved C(sp3)-H functionalization with dearomatization provides a promising platform for the construction of structurally diverse molecules.
Tetrahydroquinazoline derivatives and synthesis method and applications thereof
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Paragraph 0052-0056, (2019/05/08)
The invention provides tetrahydroquinazoline derivatives and a synthesis method and applications thereof. The synthesis method is characterized by comprising following steps: carrying out aromatic ring nucleophilic substitution reactions between substitut
Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders
Cisar, Justin S.,Weber, Olivia D.,Clapper, Jason R.,Blankman, Jacqueline L.,Henry, Cassandra L.,Simon, Gabriel M.,Alexander, Jessica P.,Jones, Todd K.,Ezekowitz, R. Alan B.,O'Neill, Gary P.,Grice, Cheryl A.
, p. 9062 - 9084 (2018/09/06)
The serine hydrolase monoacylglycerol lipase (MGLL) converts the endogenous cannabinoid receptor agonist 2-arachidonoylglycerol (2-AG) and other monoacylglycerols into fatty acids and glycerol. Genetic or pharmacological inactivation of MGLL leads to elevation in 2-AG in the central nervous system and corresponding reductions in arachidonic acid and eicosanoids, producing antinociceptive, anxiolytic, and antineuroinflammatory effects without inducing the full spectrum of psychoactive effects of direct cannabinoid receptor agonists. Here, we report the optimization of hexafluoroisopropyl carbamate-based irreversible inhibitors of MGLL, culminating in a highly potent, selective, and orally available, CNS-penetrant MGLL inhibitor, 28 (ABX-1431). Activity-based protein profiling experiments verify the exquisite selectivity of 28 for MGLL versus other members of the serine hydrolase class. In vivo, 28 inhibits MGLL activity in rodent brain (ED50 = 0.5-1.4 mg/kg), increases brain 2-AG concentrations, and suppresses pain behavior in the rat formalin pain model. ABX-1431 (28) is currently under evaluation in human clinical trials.
Direct Intermolecular C-H Functionalization Triggered by 1,5-Hydride Shift: Access to N-Arylprolinamides via Ugi-Type Reaction
Zhen, Le,Wang, Jiankun,Xu, Qing-Long,Sun, Hongbin,Wen, Xiaoan,Wang, Guangji
supporting information, p. 1566 - 1569 (2017/04/13)
A novel Ugi-type reaction triggered by 1,5-hydride shift has been established, giving access to N-arylprolinamides and related compounds in high atom economy and good yields. This is an example of a two starting material-three component reaction. The benz
CARBAMATE COMPOUNDS AND OF MAKING AND USING SAME
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Paragraph 00236, (2013/07/19)
This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compunds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
Synthesis of fused indazole ring systems and application to nigeglanine hydrobromide
Sather, Aaron C.,Berryman, Orion B.,Rebek, Julius
supporting information; experimental part, p. 1600 - 1603 (2012/06/05)
The single-step synthesis of fused tricyclic pyridazino[1,2-a]indazolium ring systems is described. Structural details revealed by crystallography explain the unexpected reactivity. The method is applied to the gram scale synthesis of nigeglanine hydrobro
Intramolecular redox-triggered C-H functionalization
Jurberg, Igor D.,Peng, Bo,Woestefeld, Eckhard,Wasserloos, Maximilian,Maulide, Nuno
supporting information; experimental part, p. 1950 - 1953 (2012/04/04)
Sacrifice for the team: A one-pot method achieves remote functionalization at the α-position of an amine moiety through the sacrificial reduction of a neighboring group. The process takes advantage of an intramolecular redox reaction, thereby avoiding the need for any external oxidants. This method was applied to a concise five-step total synthesis of indolizidine 167B.
