📜氯苯置于magnesium,Selenium,盐酸体系中,用 乙醚,水 作为反应溶剂,化学反应 7.0H,以68.4 G的收率获得产物苯硒酚 参考文献:셀레놀류의 제조 방법 标题:셀레놀류의 제조 방법 摘要:本发明的主要目的是提供一种在每个生产批次中产率变化小且具有高产率的生产硒醇的方法.该目的通过包括以下过程1和2的硒醇的生产方法来实现.过程1:通过使得表示为通式(1)的格里纳尔试剂与硒发生反应,获得含有表示为通式(2)的硒镁卤化物的反应物的过程;过程2:将从过程1获得的反应物在酸性溶液中处理,反应生成表示为通式(3)的硒醇的过程.
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-9034844-B2 优先权日:2009-04-06 标 题 :6′-sialyllactose salts and process for their synthesis and for the synthesis of other alpha-sialyloligosaccharides 发明人:TAMERLANI GIANCARLO; LOMBARDI ILARIA; BARTALUCCI DEBORA; DANESI ANDREA; SALSINI LIANA; MANONI MARCO; CIPOLLETTI GIOVANNI 权利人:TAMERLANI GIANCARLO; LOMBARDI ILARIA; BARTALUCCI DEBORA; DANESI ANDREA; SALSINI LIANA; MANONI MARCO; CIPOLLETTI GIOVANNI; INALCO SPA 摘要:The present invention relates to a process of synthesis of α-sialyl oligosaccharides and in particular of 6′-sialyllactose and its salts comprising a step of coupling by Koenigs-Knorr reaction under conditions that allow its use on an industrial scale.
专利号:US-6005097-A 优先权日:1996-06-14 标题 :Processes for high-yield diastereoselective synthesis of dideoxynucleosides 发明人:CHEN SHU-HUI; LI XIUYAN 权利人:VION PHARMACEUTICALS INC 摘要:The present invention relates to methods for substantially enhancing the stereoselective synthesis of β-anomeric nucleoside analogs. In methods according to the present invention, the introduction of a phenylseleno group onto a blocked lactone sugar precursor may be selected so that the desirable phenylseleno substituent is introduced on the side of the blocked lactone away from the blocking group. This stereospecific introduction of the phenylseleno group in sugar precursor allows the synthesis of nucleoside analogs and in particular, 2',3',-dideoxy- and 2',3'-dideoxy-2',3'-didehydronucleoside analogs in very high yield. In certain preferred embodiments, the preferred phenylseleno blocked lactone is obtained in an amount representing approximately 90% or more of the total amount of the stereoisomers obtained. In even more preferred embodiments, the amount of the preferred stereoisomer is at least 95%, even more preferably at least about 97% of the total amount of phenylseleno blocked lactone produced.
专利号:US-6069250-A 优先权日:1995-12-14 标 题 :Method and compositions for the synthesis of dioxolane nucleosides with β-configuration 发明人:MANSOUR TAREK; CIMPOIA ALEX; BEDNARSKI KRZYSZTOF 权利人:IAF BIOCHEM INT 摘要:The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about -10 DEG C. wherein R1 and L are as defined herein.
专利号:US-4762935-A 优先权日:1986-10-06 标题:Precursors and synthesis of methyl-9-oxo-11α,16-dihydroxy-16-vinyl-5-cis-13-trans-prostadienoates 发明人:WISSNER ALLAN; GREEN KENNETH E; HAMANN PHILIP R; LEVIN JEREMY 权利人:AMERICAN CYANAMID CO 摘要:This disclosure describes novel compounds which are useful as precursors in the synthesis of 9-oxo-11α,16-dihydroxy-16-vinyl-5-cis-13-trans-prostadienoate esters which possess activity as hypotensive agents and/or as vasodilators.
专利号:US-2014234364-A1 优先权日:2011-09-23 标 题:Total synthesis and immunological evaluation of saccharide moieties of the lipopolysaccharide from neisseria meningitidis 发明人:SEEBERGER PETER H; YANG YOU; ANISH CHAKKUMKAL; REINHARDT ANIKA 权利人:MAX PLANCK GES ZUR FÖRDERUNG DER WISSENSCHAFTEN E V 摘要:The present invention relates to the total chemical synthesis of the monosaccharide 35 # (R′â•?H), the disaccharide 36 # (R′≠H; R″â•?H), the trisaccharide 37 # (R′≠H; R″≠H; R′″≠H) and the tetrasaccharide 1 # (R′≠H; R″≠H; R′″≠H) of the following general formula wherein R represents —Y—NH 2 Y represents a linker R′ is H or R″ is H or R′″ is H or of the lipopolysaccharide from Neisseria meningitidis , as well as to the trisaccharide 37 # and the tetrasaccharide 1 # , to vaccines containing at least one of the saccharides 1 # , 35 # , 36 # , and 37 # and to the use of such vaccine for immunization against diseases caused by infection with bacteria containing the tetrasaccharide α-GlcNAc-(1→2)-α-Hep-( 1→3 )-α-Hep-(1→5)-α-Kdo or the trisaccharide α-Hep-(1→3)-α-Hep-(1→5)-α-Kdo or α-GlcNAc-(1→2)-±-Hep-(1→3)-α-Hep, especially for immunization against meningitis, septicaemia, pneumonia and nasopharyngitis caused by Neisseria meningitidis.