📜8-溴辛酸乙酯置于sodium Phosphinate,水,Sodium Hexamethyldisilazane,Sodium Hydroxide体系中,用 四氢呋喃 作为反应溶剂,化学反应 25.0H,反应生成 肉豆蔻油酸 参考文献:Synthesis And Characterization Of Novel Acyl-Glycine Inhibitors Of Glyt2 标题:Synthesis And Characterization Of Novel Acyl-Glycine Inhibitors Of Glyt2 摘要:It Has Been Demonstrated Previously That The Endogenous Compound N-Arachidonyl-Glycine Inhibits The Glycine Transporter Glyt2,Stimulates Glycinergic Neurotransmission,And Provides Analgesia In Animal Models Of Neuropathic And Inflammatory Pain. However,It Is A Relatively Weak Inhibitor With An Ic50,Of 9 Mu M And Is Subject To Oxidation Via Cyclooxygenase,Limiting Its Therapeutic Value. In This Paper We Describe The Synthesis And Testing Of A Novel Series Of Monounsaturated C18 And C16 Acyl-Glycine Molecules As Inhibitors Of The Glycine Transporter Giyt2. We Demonstrate That They Are Up To 28 Fold More Potent That N-Arachidonyl-Glycine With No Activity At The Closely Related Glyt1 Transporter At Concentrations Up To 30 Mu M. This Novel Class Of Compounds Show Considerable Promise As A First Generation Of Giyt2 Transport Inhibitors. DOI:10.1021/acschemneuro.7B00105
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-9643915-B2 优先权日:2013-03-15 标题:Methods for the synthesis of sphingomyelins and dihydrosphingomyelins 发明人:ONICIU DANIELA CARMEN; HECKHOFF STEFAN; OSWALD BENOIT; REBMANN PETER; PEER ANDREAS; GONZALEZ MIGUEL; SAUTER PATRIK 权利人:CERENIS THERAPEUTICS HOLDING SA 摘要:The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
专利号:US-9708354-B2 优先权日:2013-03-15 标 题:Methods for the synthesis of sphingomyelins and dihydrosphingomyelins 发明人:ONICIU DANIELA CARMEN; HECKHOFF STEFAN; OSWALD BENOIT; REBMANN PETER; PEER ANDREAS; GONZALEZ MIGUEL; SAUTER PATRIK 权利人:CERENIS THERAPEUTICS HOLDING SA 摘要:The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
专利号:US-7910623-B2 优先权日:2005-07-22 标 题 :Synthesis of scabronines and analogues thereof 发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P 权利人:SLOAN KETTERING INST CANCER 摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-9884830-B2 优先权日:2004-05-21 标题 :Synthesis of tetracyclines and analogues thereof 发明人:MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.
1: Quan LH, Zhang C, Dong M, Jiang J, Xu H, Yan C, Liu X, Zhou H, Zhang H, Chen L, Zhong FL, Luo ZB, Lam SM, Shui G, Li D, Jin W. Myristoleic acid produced by enterococci reduces obesity through brown adipose tissue activation. Gut. 2020 Jul;69(7):1239-1247. doi: 10.1136/gutjnl-2019-319114. Epub 2019 Nov 19. 768:189-98. doi: 10.1016/j.ejphar.2015.10.053. Epub 2015 Oct 31. 29(2):211-219. doi: 10.4062/biomolther.2020.169. 4: Kim YG, Lee JH, Lee J. Antibiofilm activities of fatty acids including myristoleic acid against Cutibacterium acnes via reduced cell hydrophobicity. Phytomedicine. 2021 Oct;91:153710. doi: 10.1016/j.phymed.2021.153710. Epub 2021 Aug 18. 47(1):59-65. doi: 10.1002/pros.1047. 586(1):96-101. doi: 10.1016/j.febslet.2011.12.004. Epub 2011 Dec 9. 22(11):1431-6. doi: 10.2116/analsci.22.1431. 293(4):200-5. doi: 10.1007/s004030000203.
合成参考文献
参考文献:10.1007/s11010-010-0403-z 摘要:Romanowicz L, Bańkowski E. Sphingolipids of human umbilical cord vein and their alteration in preeclampsia. Molecular and Cellular Biochemistry. 2010 Feb 14;340(1-2):81–9. doi: 10.1007/s11010-010-0403-z. 参考文献:10.1007/s00709-011-0303-4 摘要:Shukla E, Singh SS, Singh P, Mishra AK. Chemotaxonomy of heterocystous cyanobacteria using FAME profiling as species markers. Protoplasma. 2012 Jul;249(3):651–61. doi: 10.1007/s00709-011-0303-4. 参考文献:10.1007/s11033-011-1190-7 摘要:Oh D, Lee Y, La B, Yeo J, Chung E, Kim Y, Lee C. Fatty acid composition of beef is associated with exonic nucleotide variants of the gene encoding FASN. Molecular Biology Reports. 2011 Jul 20;39(4):4083–90. doi: 10.1007/s11033-011-1190-7.