专利号:US-6350878-B1 优先权日:1998-05-18 标 题 :Intermediates for the synthesis of epothilones and methods for their preparation 发明人:ALTMANN KARL-HEINZ; BAUER ARMIN; SCHINZER DIETER 权利人:NOVARTIS AG 摘要:The invention relates to a method of synthesis for a compound of formula (I),wherein R is a heterocyclyl moiety and X1, X2, X3 and X4 are, independently of each other, protecting groups, which is appropriate for the synthesis of epothilone B and desoxyepothione B.
专利号:US-6849743-B2 优先权日:1997-08-15 标 题 :Synthesis of clasto-lactacystin β-lactone and analogs thereof 发明人:SOUCY FRANCOIS; FLAMONDON LOUIS; BEHNKE MARK; ROUSH WILLIAM 权利人:MILLENNIUM PHARM INC 摘要:The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.
专利号:US-2009306400-A1 优先权日:2006-03-27 标 题:Convergent process for the synthesis of taxane derivatives. 发明人:HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING 权利人:HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING 摘要:The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds, including taxane derivatives, and convergent processes for the preparation of these taxane derivatives and their intermediates.
专利号:US-4803287-A 优先权日:1986-04-16 标题 :Certain photochromic fulgide compounds and method for their synthesis 发明人:HIBINO JUNICHI; ANDO EIJI 权利人:AGENCY IND SCIENCE TECHN 摘要:The invention provides a photochromic material characterized by an improvnt in balance of the substituents in the conventional furylfulgides and represented by the general formula: ##STR1## (wherein R represents an alkyl chain having 5 to 31 carbon atoms). According to this molecular structure, a mutually appropriate steric hindrance is induced between the isopropylidence group and the long-chain alkyl group to make the regio isomer unstable, thus preventing the regio isomer from being by-produced while also inhibiting any isomerization reaction from occuring in the synthesis of the fulgide. Further, a good balance of hydrophilic part and hydrophobic part is produced to facilitate formation of a Langmuir-Blodgett film.
专利号:US-3959322-A 优先权日:1960-09-22 标 题:Synthesis of 13-alkyl-gon-4-ones 发明人:HUGHES GORDON ALAN; SMITH HERCHEL 权利人:SMITH HERCHEL 摘要:The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.
专利号:US-6417399-B1 优先权日:1997-01-14 标 题:Amelioration of neurological disorders by the administration of (2R),(3S), and/or (2S),3(S) stereoisomers of valnoctamide 发明人:BIALER MEIR; YAGEN BORIS; SPIEGELSTEIN OFER; ROEDER MICHAEL; SCHURIG VOLKER 权利人:YISSUM RES DEV CO 摘要:The present invention generally relates to the individual stereoisomers of the drug valnoctamide (a mixture of four stereoisomer kinds, VCD-valmethamide or 2-ethyl-3-methyl pentanamide) useful in treatment of neurological and psychotic disorders such as different kinds of epilepsy and affective disorders, and useful as tranquilizers and to treat pain, and to pharmaceutical compositions containing, as an active ingredient, these stereoisomers. The present invention further relates to a method for stereoselective separation and quantification of the four stereoisomers from a racemic mixture of VCD or plasma of patients treated with the racemic drug. The present invention further relates to a unique method for the synthesis of the individual stereoisomers.
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