专利号:US-9862745-B2 优先权日:2004-03-30 标题 :Synthesis of boronic ester and acid compounds 发明人:AMMOSCATO VINCE; BISHOP JOHN E; CHIU FANG-TING; GEISER ACHIM; GOMEZ JEAN-MARC; HETT ROBERT; KOELLNER CHRISTOPH; KULKARNI VITHALANAND R; LO YOUNG; MUNK STEPHEN; PICKERSGILL I FRASER 权利人:MILLENNIUM PHARM INC; MILLENNIUM PHARM INC 摘要:The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.
专利号:EP-0113566-A1 优先权日:1982-12-20 标题:New intermediate compounds for synthesis of aklavinones and their preparation 发明人:KISHI YOSHITO 权利人:MEIJI SEIKA KAISHA 摘要:A new compound of the formulan wherein R, is a hydrogen atom, a hydroxyl group or an alkoxyl group of 1-4 carbon atoms and R 2 is an alkyl group of 1-4 carbon atoms is now provided. This new compound is useful as intermediate for synthesis of aklavinones which may be coupled with sugars, for example, daunosamine to give anthracycline antibiotics. The new compound of this invention is produced by several reaction steps started from a 3-halo-5-substituted or unsubstituted naphthoquinone and a furan diene compound. This process involves new regiospecific Diels-Alder condensation and new asymmetric crossed aldol condensation.
专利号:US-8067465-B2 优先权日:2002-01-15 标题:Tricyclic-bis-enone derivatives and methods of use thereof 发明人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO 权利人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO; DARTMOUTH COLLEGE 摘要:Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.
专利号:US-11674160-B2 优先权日:2018-06-19 标题:Materials and methods for the synthesis of carbon products from non-biosynthetic processes and streams 发明人:SMITH GARY; PEARLMAN PAUL S; KIRBY GREGORY S 权利人:INV NYLON CHEMICALS AMERICAS LLC 摘要:Methods, systems and compositions for producing at least one light-boiling, volatile, organic product using at least a portion of one or more carbon containing substances from a non-biosynthetic process in a biosynthetic process are provided. These methods, systems and compositions are useful in reducing waste treatment load of carbon containing chemical process waste streams.
专利号:US-2017349919-A1 优先权日:2014-12-19 标题 :Micro-organism for the production of stereo-specific s, s-2,3-butanediol 发明人:SOLEM CHRISTIAN; JENSEN PETER RUHDAL; CHEN JUN; LIU JIANMING 权利人:UNIV DANMARKS TEKNISKE 摘要:The invention relates to a genetically modified lactic acid bacterium capable of producing (S,S)-2,3-butanediol stereo specifically from glucose under aerobic conditions. Additionally the invention relates to a method for producing (S,S)-2,3-butanediol and L-acetoin using the genetically modified lactic acid bacterium, under aerobic conditions in the presence of a source of iron-containing porphyrin or a source of metal ions (Fe 3+ /Fe 2+ ). The lactic acid bacterium is genetically modified to express heterologous genes encoding enzymes catalysing the stereo-specific synthesis of (S,S)-2,3-butandiol; and additionally a number of genes are deleted in order to maximise the production of (S,S)-2,3-butanediol as compared to other products of oxidative fermentation.
专利号:US-6872856-B2 优先权日:2000-06-28 标 题 :Cyclic ketones, their preparation and their use in the synthesis of amino acids 发明人:BLAKEMORE DAVID CLIVE; BRYANS JUSTIN STEPHEN 权利人:WARNER LAMBERT CO 摘要:A method is provided for making an enantiomerically pure compound of the formula: in which R and R′ represent C1?C10 alkyl, C2?C10 alkenyl or C3?C10 cycloalkyl and the wedges signify (S)- or (R)-stereochemistry, the substituents in compound (II) being trans. Conjugate addition is carried out between an organometallic nucleophile that provides a group R as defined above and (R)-4-acetoxycyclopent-2-en-1-one, (S)-4-acetoxycyclopent-2-en-1-one or a similar compound in which acetoxy is replaced by another leaving group to give, e.g. in the case of the acetoxy compound, a trans 3,4-disubstituted addition product of formula III or IV; The acetyl group is eliminated from the addition product to give an (R)- or (S)-4-alkyl or 4-alkenyl cyclopent-2-en-1-one the compound of formula is then to be hydrogenated to give a cyclopentanone of formula (I) or conjugate addition of a second organometallic nucleophile that provides a group R′ as defined above to the compound of the above formula may be carried out to give a trans 3,4-disubstituted addition product of formula (II). One of the above compounds may be converted e.g. via an intermediate (XV)-(XVIII) (in which the substituents R and R′ and the wedges have the meanings indicated above) to a gabapentin analogue of one of the formulae shown below: in which the substituents R and R′ and the wedges also have the meanings indicated above.