📜5-Phenoxymethyl-1,2,3-Oxadiazole 3-Oxide置于palladium 10% On Activated Carbon,氢气体系中,用 甲醇 作为反应溶剂,20.0 °C,101.33 Kpa 条件下,反应 2.0H,以98%的收率获得产物苯氧基丙酮 参考文献:Reaction Of 1,2,3-Oxadiazole 3-Oxides 标题:Reaction Of 1,2,3-Oxadiazole 3-Oxides 摘要:1,2,3-Oxadiazole 3-Oxides With An Alkoxymethyl Group At The 5-Position Were Reduced By Reacting Them With Sodium Borohydride To Produce 4,5-Dihydro-1,2,3-Oxadiazole 3-Oxides In Good Yields,Which Were Further Transformed Into Substituted Diazene N-Oxides By Reacting With Grignard Reagents. DOI:10.3987/com-12-S(N)127
专利号:US-3954709-A 优先权日:1973-05-29 标 题:Phenylethyl group containing resins for the synthesis of peptides 发明人:STEWART JOHN M; MATSUEDA GARY R 权利人:UNIV COLORADO 摘要:The phenylethyl group, ##SPC1## n In polymer carriers for the synthesis of peptides and peptide amides, particularly polymer carriers such as styrene-1% divinyl benzene polymers for use in solid phase peptide synthesis. n The invention described herein was made in the course of work under a grant or award from the Department of Health, Education and Welfare.
专利号:US-2003180804-A1 优先权日:2001-10-29 标题:Solid phase synthesis of chemical libraries 发明人:PRYOR KENT E; LEWIS RONALD D; BROWN JASON W 权利人:CORVAS INT INC 摘要:The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.
专利号:US-6492136-B1 优先权日:1995-12-07 标题 :Solid phase organic synthesis 发明人:FLITSCH SABINE LAHJA; TURNER NICHOLAS JOHN 权利人:GENZYME LTD 摘要:A method of synthesis of a material corresponding to the general formula:characterized in that it comprises a material corresponding to the following general formula:being cleaved as indicated enzymatically or non-enzymatically using acid catalysis in the presence of a nucleophile, wherein: R1 represents a group providing the site for exo-enzyme or acid hydrolysis; R2 represents an intermediate linked to a solid support; R3 represents a carbohydrate, (oligo-)saccharide, (glyco-)peptide, (glyco-)lipid or an organic molecule which is at least one of heterocyclic and aromatic in structure; X represents O, N(H), N(R''), C(O)O, S, C(O)N(H) or C(O)N(R''), R'' being a non-interfering group; and Support represents a solid support.
专利号:WO-2006052263-A1 优先权日:2004-11-10 标题:Synthesis and separation of optically active isomers and cyclopropyl derivatives of spironolactone and their biological action 发明人:RANADE VASANT V; SOMBERG JOHN CHARIN 权利人:RANADE VASANT V 摘要:Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effects mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and in the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in
专利号:US-2009325918-A1 优先权日:2008-06-16 标 题:Synthesis and separation of optically active isomers and cyclopropyl derivatives of spironolactone and their biological action 发明人:SOMBERG JOHN C; RANADE VASSANT V 权利人:SOMBERG JOHN C; RANADE VASSANT V 摘要:Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effect mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and it the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in men.
专利号:US-7479387-B2 优先权日:2000-11-08 标题 :Compositions and methods for the synthesis and subsequent modification of uridine-5′-diphosphosulfoquinovose (UDP-SQ) 发明人:BENNING CHRISTOPH; SANDA SHERRIE LEA; YU BIN 权利人:UNIV MICHIGAN STATE 摘要:The present invention is directed to compositions and methods related to the synthesis and modification of uridine-5′-diphospho-sulfoquinovose (UDP-SQ). In particular, the methods of the present invention comprise the utilization of recombinant enzymes from Arabidopsis thaliana , UDP-glucose, and a sulfur donor to synthesize UDP-SQ, and the subsequent modification of UDP-SQ to form compounds including, but not limited to, 6-sulfo-α-D-quinovosyl diaclyglycerol (SQDG) and alkyl sulfoquinovoside. The compositions and methods of the invention provide a more simple, rapid means of synthesizing UDP-SQ, and the subsequent modification of UDP-SQ to compounds including, but not limited to, SQDG.
1: Dafforn A, Neenan JP, Ash CE, Betts L, Finke JM, Garman JA, Rao M, Walsh K, Williams RR. Acetylcholinesterase inhibition by the ketone transition state analog phenoxyacetone and 1-halo-3-phenoxy-2-propanones. Biochem Biophys Res Commun. 1982 Jan 29;104(2):597-602.
合成参考文献
摘要:Xu, L.; Wu, X.; Xiao, J., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 303. 摘要:De Wildeman, S.; Sereinig, N., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 166. 摘要:Huang, Y.; Dömling, A., Science of Synthesis: Multicomponent Reactions, (2013) 1, 532. 摘要:Simon, R. C.; Busto, E.; Fischereder, E.-M.; Fuchs, C. S.; Pressnitz, D.; Richter, N.; Kroutil, W., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 392. 摘要:Simon, R. C.; Busto, E.; Fischereder, E.-M.; Fuchs, C. S.; Pressnitz, D.; Richter, N.; Kroutil, W., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 398.