专利号:US-6995289-B2 优先权日:2000-08-02 标题 :Process for synthesis of alpha, beta-unsaturated ketones 发明人:PATEL IAN; HOPES PHILIP 权利人:ASTRAZENECA AB 摘要:A method for the synthesis of an α,β-unsaturated ketone useful for making substituted 1,4-dihydropyridines is described by reacting an aldehyde with pyrrolidine and then adding a ketone followed by trifluoroacetic acid at low temperature. The synthesis is used in a process for making substituted 1,4-dihydropyridines wherein a vinylogous amide is prepared by reacting a 1,3-cyclohexanedione with a phenylethylamine. The α,β-unsaturated ketone can be reacted with a vinylogous amide to form a 1,5-diketone which can be converted to a substituted 1,4-dihydropyridine.
专利号:EP-1721894-A1 优先权日:2005-05-13 标题 :Process for the synthesis of prostaglandin derivatives 发明人:LISI GIUSEPPE 权利人:TECHNOPHARMA SA 摘要:An alternative method for the synthesis of prostaglandin F analogues, in particular, analogues of PGF 2α and specifically for the synthesis of latano-prost, wherein the transformation of the lactone intermediate (5)n ninto the corresponding lactol (7)n nis carried out by treating the lactone intermediate (5) with a silane, preferably polymethylhydrosiloxane (PMHS), in the presence of a titanocene - and preferably titanocene fluoride. n The method enables considerable production economies with respect to the conventional reduction of lactone with diisobutylaluminum hydride (DIBAL-H).
专利号:US-2013184465-A1 优先权日:2010-09-30 标 题:Process for the synthesis of thio-triazolo-group containing compounds 发明人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL 权利人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL; BASF SE 摘要:The present invention relates to a process using specific magnesium reagents for providing thio-triazolo group-containing compounds and for the synthesis of precursors therefor. The invention furthermore relates to intermediates and to their preparation.
专利号:US-9453044-B2 优先权日:2012-02-07 标题 :Method of synthesizing peptides, proteins and bioconjugates 发明人:LIU CHUAN FA; ZHAO JUNFENG 权利人:UNIV NANYANG TECH 摘要:The invention relates to the synthesis of peptides, proteins and related bioconjugates, and in particular, to such synthesis using a peptide ligation method whereby a C-terminal salicylaldehyde ester peptide is reacted with an aminoacyl-N-hydroxl peptide. The invention also relates to the synthesis of cyclic peptides, including serinyl- or threonyl-containing cyclic peptides. The invention further relates to a solid phase synthesis of C-terminal salicylaldehyde ester peptides.
专利号:US-6048991-A 优先权日:1990-11-16 标题:Preparation of epoxides 发明人:HAERMELING DIETER 权利人:BASF AG 摘要:Alpha-hydroxy-epoxides of alpha-alkoxy-epoxides of the formula IV ##STR1## in which the substituents have the following meanings: R 7 , R 8 , R 9 , R 10 , R 11 are independently hydrogen, C 1 -C 20 -alkyl, C 3 -C 12 -cycloalkyl, C 4 -C 20 -cycloalkylalkyl, C 1 -C 20 -hydroxy-alkyl, a heterocyclic ring, or an aryl or C 7 -C 20 -arylalkyl group optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, halogen, C 1 -C 4 -haloalkyl, C 1 -C 4 -halo-alkoxy, phenyl, phenoxy, halophenyl, halophenoxy, carboxy, C 2 -C 8 -alkoxycarbonyl, or cyano, or R 7 and R 8 or R 7 and R 9 or R 7 and R 10 or R 9 and R 10 or R 10 and R 11 together form a (CH 2 ) n group in which n is an integer from 1 to 10 and which may be optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, and/or halogen, and n R 12 is hydrogen, C 1 -C 8 -alkyl, or benzyl, n provided that R 10 is not hydrogen, methyl, ethyl, propyl, or cyclohexyl when R 7 , R 8 , R 9 , or R 11 is hydrogen, that R 7 is not methyl when R 8 is methyl or phenyl and R 9 , R 10 , or R 11 is hydrogen, that R 7 is not methyl when R 8 , R 9 , R 10 , or R 11 is hydrogen and R 12 is ethyl, that R 7 is not phenyl or hexyl when R 8 , R 9 , R 10 , or R 11 is hydrogen, that R 9 is not methyl when R 7 , R 8 , R 10 , or R 11 is hydrogen, that R 10 and R 11 are not methyl when R 7 , R 8 , or R 9 is hydrogen, and that R 7 and R 10 do not together form an unsubstituted cycloalkyl when R 8 , R 9 , or R 11 is hydrogen. The epoxides of the above formula serve as intermediates for the synthesis of, inter alia, perfumes, plant protectants and polymers.
专利号:US-10266503-B1 优先权日:2016-05-24 标 题 :Sulfoxide ligand metal catalyzed oxidation of olefins 发明人:WHITE M CHRISTINA; AMMANN STEPHEN E; LIU WEI; MA RULIN 权利人:UNIV ILLINOIS 摘要:The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp 3 )-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.