专利号:US-9464021-B2 优先权日:2013-11-01 标题 :Method of preparation of stereospecific quinone derivatives 发明人:MEHTA DILIP S; MOHAN PRIYA; SHASTRI MAYANK; REID TED 权利人:MEHTA DILIP S; MOHAN PRIYA; SHASTRI MAYANK; REID TED 摘要:The description provides processes for the regio and stereospecific synthesis of polyprenylatedquinone derivatives, such as Vitamin K1, K2 and Ubiquinone, exploiting dithioacetals, especially 1,3-dithiane, mediated Umpolung chemistry which works along a new concept “Inhibiting resonance delocalization (IRD)†to overcome isomerization generated due to delocalization of allyliccarbanion on the Ï€-electron cloud of an allylic systems by the conventional synthesis.
专利号:US-5231232-A 优先权日:1991-12-18 标题 :Method of preparing C-18 ketones used in the manufacture of Vitamins E and K 发明人:BABLER JAMES H 权利人:UNIV LOYOLA CHICAGO 摘要:Methods of forming unsaturated C-18 ketones which can be used in the synthesis of Vitamins E and K 1 are disclosed. One procedure involves coupling a C-9 primary allylic halide to a carbonyl-group-containing C-9 terminal alkyne. A second, two-step procedure employs a C-4 bis allylic halide (molar excess) and a carbonyl-group-containing C-9 terminal alkyne to form a C-13 primary allylic halide. The C-13 primary allylic halide can then be converted to the desired C-18 ketone by reaction with 2-methyl-3-butyn-2-ol. Novel C-18 ketones (e.g., 14-hydroxy-6,14-dimethyl-10-methylene-5-pentadecen-7,12-diyn-2-one), C-13 allylic halides (e.g., 10-chloromethyl-6-methyl-5,10-undecadien-7-yn-2-one) and C-9 allylic halides (e.g., 6-chloromethyl-2-methyl-6-hepten-3-yn-2-ol) are formed in the process.
专利号:US-6610844-B2 优先权日:1996-12-11 标题:Processes for preparation of 9,11-epoxy steroids and intermediates useful therein 发明人:NG JOHN S; LIU CHIN; ANDERSON DENNIS K; LAWSON JON P; WIECZOREK JOSEPH; KUNDA SASTRY A; LETENDRE LEO J; POZZO MARK J; SING YUEN-LUNG L; WANG PING T; YONAN EDWARD E; WEIER RICHARD M; KOWAR THOMAS R; BAEZ JULIO A; ERB BERNHARD 权利人:SEARLE & CO 摘要:Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula Iwherein-A-A- represents the group -CHR4-CHR5- or -CR4=CR5-;R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano and aryloxy;R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical;-B-B- represents the group -CHR6-CHR7- or an alpha- or beta-oriented group:where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; andR8 and R9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.
专利号:US-7220870-B2 优先权日:1995-03-14 标 题:Hydrolytic kinetic resolution of cyclic substrates 发明人:JACOBSEN ERIC N; TOKUNAGA MAKOTO; LARROW JAY F 权利人:HARVARD COLLEGE 摘要:The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
专利号:US-7129345-B2 优先权日:1995-12-11 标题:Keto-substituted steroid compounds 发明人:NG JOHN S; WANG PING T; BAEZ JULIO A; LIU CHIN; ANDERSON DENNIS K; LAWSON JON P; ERB BERNHARD; WIECZOREK JOSEPH; MUCCIARIELLO GENNARO; VANZANELLA FORTUNATO; KUNDA SASTRY A; LETENDRE LEO J; POZZO MARK J; SING YUEN-LUNG L; YONAN EDWARD E 权利人:PHARMACIA CORP 摘要:Multiple novel keto-substituted intermediates are provided for the synthesis of epoxymexrenone, useful as an Aldosterone Receptor Antagonist.
专利号:US-4898875-A 优先权日:1986-09-04 标题:Mercapto-substituted hydroxyethyl-(triazol-l-yl) derivatives 发明人:BUECHEL KARL H; HOLMWOOD GRAHAM; KRAATZ UDO; KRAEMER WOLFGANG; REINECKE PAUL; BRANDES WILHELM; STENDEL WILHELM 权利人:BAYER AG 摘要:Novel mercapto-substituted hydroxyethyl-(triazol-l-yl) derivatives of the formula (I) in which Ar represents optionally substituted aryl, X represents oxygen, sulphur, a direct bond or the groupings -CH2-, -CH2-CH2-, -O-CH2-, -SCH2-, -O-CH2-CH2-, and -S-CH2-CH2-, the hetero atom being bonded to the aryl radical if X represents -OCH2-, -SCH2-, -O-CH2-CH2- or -S-CH2-CH2- and R represents hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl or optionally substituted phenyl, and their acid addition salts and metal salt complexes are very effective as fungicides and parasiticides. Novel oxiranes of the formula in which Ar and X have the above-mentioned meaning, and their use as intermediates for the synthesis of the mercapto-substituted hydroxyethyl-(triazol-l-yl) derivatives.
参考标题:Divergent Enantioselective Synthesis Of (−)-Galanthamine And (−)-Morphine 作者:Barry M. Trost,Weiping Tang,F. Dean Toste |发布日期:2005.10.1 摘要:Tricyclic Intermediate Is Available In Six Steps From 2-Bromovanillin And The Monoester Of Methyl 6-Hydroxycyclohexene-1-Carboxylate. This Intermediate Requires Only Two Steps To Convert To (-)-Galanthamine. Using A Heck Vinylation, We Found That The Fourth Ring Of Codeine/morphine Could Be Formed. The Final Ring Formation Involves A Novel Visible Light-Promoted Hydroamination. Thus, Six Steps Are Required
合成参考文献
摘要:Lindenschmidt, A., Science of Synthesis, (2007) 25, 269. 摘要:Aggarwal, V. K.; Crimmin, M.; Riches, S., Science of Synthesis, (2008) 37, 331. 摘要:Tang, Y.; Sun, X.-L., Science of Synthesis, (2008) 39, 503.