专利号:US-4049710-A 优先权日:1976-02-24 标题:Novel carbamimidoyl chlorides and their use in the synthesis of herbicidal triazinediones 发明人:TOCKER STANLEY 权利人:DU PONT 摘要:Carbamimidoyl chlorides of the formula: WHERE R2 is alkyl of 1-4 carbon atoms are useful as intermediates in the synthesis of herbicidal triazinediones of the formula: where R1 is certain organic radicals.
专利号:WO-2023086801-A1 优先权日:2021-11-09 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:WO-2020248279-A1 优先权日:2019-06-14 标 题 :Continuous synthesis method for substituted benzoate organic matter 发明人:HONG HAO; LU JIANGPING; ZHANG ENXUAN; LIU ZHIQING; LI CHAO 权利人:JINLIN ASYMCHEM LABORATORIES CO LTD 摘要:The present invention provides a continuous synthesis method for a substituted benzoate organic matter. The continuous synthesis method comprises: in the presence of a catalyst and an organic solvent, continuously feeding an organic matter as represented by formula (I) and oxygen into a continuous reaction device for continuous oxidation reaction to obtain a substituted benzoate organic matter, and performing continuous discharge, wherein the substituted benzoate organic matter has a structure as represented by formula (II). Oxygen is a green reagent, and is cheap and easy to obtain; the present invention would not produce a large amount of waste gas, waste water, and waste residues after the completion of reaction, and the system is easy to handle. The use of continuous reaction operation can reduce the risk of solvent flash evaporation explosion due to high concentration oxygen in batch reactions. Under the same oxidation conditions, the use of a continuous preparation process can reduce the escape of oxygen, greatly increase the utilization of oxygen, simplify the operation, and improve the reaction safety and the yield of substituted benzoate organic matters.
专利号:US-2012077802-A1 优先权日:2009-06-10 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
专利号:US-12336981-B2 优先权日:2010-09-03 标题 :Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; DRAGOVICH Peter; GOSSELIN FRANCIS; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; ROTH BRUCE; SMITH CHASE C; WANG ZHONGGUO; YUEN PO-WAI; ZHENG XIAOZHANG 权利人:VALO HEALTH INC; GENENTECH INC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
专利号:US-9771356-B2 优先权日:2012-09-21 标题 :Inhibitors of beta-hydroxylase for treatment of cancer 发明人:WANDS JACK R; DE LA MONTE SUZANNE; AIHARA ARIHIRO; OLSEN MARK JON; THOMAS JOHN-MICHAEL 权利人:RHODE ISLAND HOSPITAL; UNIV MIDWESTERN 摘要:The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydroxylase (e.g., Asparatyl (asparaginyl) β-hydroxylase (ASPH)), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.
[参考文献]: S Ramalingam, Et Al. Ft-Ir And Ft-Raman Spectra And Vibrational Investigation Of 4-Chloro-2-Fluoro Toluene Using Ab Initio Hf And Dft (B3Lyp/b3Pw91) Calculations. Spectrochim Acta A Mol Biomol Spectrosc. 2011 Jan;78(1):429-36.
合成参考文献
参考文献:10.1055/s-0036-1591523 摘要:Stradiotto M, Sawatzky R. (DPEPhos)Ni(mesityl)Br: An Air-Stable Pre-Catalyst for Challenging Suzuki–Miyaura Cross-Couplings Leading to Unsymmetrical Biheteroaryls. Synlett. 2018 Jan 02;29(06):799–804. doi: 10.1055/s-0036-1591523.