专利号:WO-9817677-A1 优先权日:1996-10-24 标 题 :Improvements in solid-phase synthesis of peptides and related compounds 发明人:ENGLEBRETSEN DARREN 权利人:UNIV QUEENSLAND; ENGLEBRETSEN DARREN 摘要:The invention relates to spacers for use in solid-phase synthesis of peptides and peptide-related compounds, in which a spacer construct is used to ensure that the target peptide or peptide-related compound is at a distance equivalent to at least 5-15 amino acids from the solid support. Constructs of the invention are particularly applicable to the synthesis of strongly hydrophobic peptide, which are otherwise difficult, if not impossible to purify and analyse. The constructs and methods of the invention are also applicable to synthesis of peptide nucleic acids.
专利号:US-2012215002-A1 优先权日:2009-10-09 标 题:Synthesis of optically active intermediate for the preparation of montelukast 发明人:LEFORT LAURENT 权利人:LEFORT LAURENT 摘要:The present invention relates to the synthesis of optically active alcohols by means of enantioselective hydrogenation of ketones in biphasic systems. In particular the present invention relates to the synthesis of an optically active alcohol of general formula (1).
专利号:US-8461357-B2 优先权日:2008-09-19 标题 :Expeditious synthesis of gibberellin A5 and esters thereof 发明人:FAIRWEATHER KELLY A; MANDER LEWIS N; PHARIS RICHARD P 权利人:FAIRWEATHER KELLY A; MANDER LEWIS N; PHARIS R P; UTI LIMITED PARTNERSHIP 摘要:An expeditious synthesis of gibberellin A 5 (GA 5 ) esters is presented, from which GA 5 may be prepared. The synthesis offers an inexpensive route of few steps to these compounds, starting from gibberellin A 3 (GA 3 ) esters in the presence of a metal hydride.
专利号:US-5549974-A 优先权日:1994-06-23 标题:Methods for the solid phase synthesis of thiazolidinones, metathiazanones, and derivatives thereof 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:The invention provides an efficient and versatile method for the combinatorial synthesis and screening of libraries of 4-thiazolidinones, metathiazanones, and derivatives thereof. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. Arrays of thiazolidinones, metathiazanones, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antihistaminic, or antimicrobial activity or use in the treatment of inflammation, hypertension, renal failure, congestive heart failure, uremia and other conditions can be prepared using this method.
专利号:US-5817751-A 优先权日:1994-06-23 标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives 发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID 权利人:AFFYMAX TECH NV 摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
专利号:EP-0439404-B1 优先权日:1990-01-25 标题 :Preparation of 2-(2'-thienyl) alkylamines and derivatives thereof and synthesis of 4,5,6,7- thieno [3,2-c] pyridine derivatives therefrom 发明人:KHATRI HIRALAL N; DEHOFF BRADLEY S 权利人:SANOFI SA 摘要:An improved process for the synthesis of 2-(2 min -thienyl)ethylamine from suitably functionalized derivatives of 2-(2 min -thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2 min -thienyl)ethylamine produced by this process is advantageously converted to the carbamic acid salt, which is suitably reconverted to 2-(2 min -thienyl)ethylamine, a useful intermediate in the synthesis of ticlopidine.
1: Huix-Rotllant M, Dumont E, Ferré N, Monari A. Photophysics of acetophenone interacting with DNA: why the road to photosensitization is open. Photochem Photobiol. 2015 Mar-Apr;91(2):323-30. doi: 10.1111/php.12395. Epub 2014 Dec 16. doi: 10.1016/j.saa.2014.12.037. Epub 2014 Dec 23. doi: 10.1021/jo500691b. Epub 2014 May 30. doi: 10.1016/j.fitote.2015.07.002. Epub 2015 Jul 6. doi: 10.1007/s00894-014-2268-7. Epub 2014 May 15. doi: 10.1107/S2053230X15002265. Epub 2015 Feb 19. 7: Casaril AM, Martinez DM, Ricordi VG, Alves D, Lenardão EJ, Schultze E, Collares T, Seixas FK, Savegnago L. Evaluation of the toxicity of α-(phenylselanyl) acetophenone in mice. Regul Toxicol Pharmacol. 2015 Dec;73(3):868-74. doi: 10.1016/j.yrtph.2015.10.004. Epub 2015 Oct 9. doi: 10.1016/j.fitote.2014.09.019. Epub 2014 Oct 5. doi: 10.4014/jmb.1506.06043. doi: 10.1021/ol5033738. Epub 2014 Dec 16. doi: 10.1155/2015/394367. Epub 2015 May 5. 12: Kouloura E, Skaltsounis AL, Michel S, Halabalaki M. Ion tree-based structure elucidation of acetophenone dimers (AtA) from Acronychia pedunculata and their identification in extracts by liquid chromatography electrospray ionization LTQ-Orbitrap mass spectrometry. J Mass Spectrom. 2015 Mar;50(3):495-512. doi: 10.1002/jms.3556. doi: 10.1002/jnr.23575. Epub 2015 Feb 22. doi: 10.1016/j.ijbiomac.2015.08.063. Epub 2015 Sep 9. doi: 10.1099/ijs.0.000170. Epub 2015 Mar 4. doi: 10.3390/molecules200611617. doi: 10.1039/c4cc08210a. Epub 2014 Nov 18. doi: 10.1007/s10482-015-0559-3. Epub 2015 Sep 5. Epub 2016 Oct 24.
合成参考文献
参考文献:10.2174/138620710791292985 摘要:Abdallah R, Grenouillet P, Vriamont N, Riant O, de Bellefon C. High throughput screening and evolution of a library of ligands in asymmetric H-transfer reduction of acetophenone. Comb Chem High Throughput Screen. 2010 Jun;13(5):393–413. doi: 10.2174/138620710791292985. 参考文献:10.1055/s-2005-871295 摘要:Chou HC, Chen JJ, Duh CY, Huang TF, Chen IS. Cytotoxic and anti-platelet aggregation constituents from the root wood of Melicope semecarpifolia. Planta Med. 2005 Nov;71(11):1078–81. doi: 10.1055/s-2005-871295. 参考文献:10.1136/thx.2010.156695 摘要:Ibrahim B, Basanta M, Cadden P, Singh D, Douce D, Woodcock A, Fowler SJ. Non-invasive phenotyping using exhaled volatile organic compounds in asthma. Thorax. 2011 Sep;66(9):804–9. doi: 10.1136/thx.2010.156695. 参考文献:10.1107/s1600536811008154 摘要:Jasinski JP, Miller WM, Samshuddin S, Narayana B, Yathirajan HS. (2E)-3-{4-[(1H-1,3-Benzimidazol-2-yl)meth-oxy]-3-eth-oxy-phen-yl}-1-(4-bromo-phen-yl)prop-2-en-1-one monohydrate. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o834–5. 参考文献:10.1107/s1600536811009214 摘要:Liu L, Li J, Shao Y. (E)-3-(1-Methyl-1H-pyrrol-2-yl)-1-phenylprop-2-en-1-one. Acta Crystallogr E Struct Rep Online. 2011 Mar 15;67(4):o894. doi: 10.1107/s1600536811009214.