📜Methyl 2-((Tert-Butoxycarbonyl)Amino)Benzoate置于lithium Hydroxide Monohydrate,水体系中,用 四氢呋喃,甲醇 作为反应溶剂,化学反应生成 2-(N-叔丁氧羰基氨基)苯甲酸 参考文献: Telomerase Reverse Transcriptase Degraders And Methods Of Use Thereof[fr] Agents De Dégradation De La Transcriptase Inverse De La Télomérase Et Leurs Procédés D'Utilisation 标题: Telomerase Reverse Transcriptase Degraders And Methods Of Use Thereof[fr] Agents De Dégradation De La Transcriptase Inverse De La Télomérase Et Leurs Procédés D'Utilisation 摘要:本公开提供了tert抑制剂化合物,一个与泛素连接酶配体相关的tert抑制剂,以及其药物组成物.本公开还提供了通过使用上述化合物和/或组成物来抑制端粒酶逆转录酶(tert)的方法,以及治疗或预防疾病或紊乱的方法.
专利号:US-2002019013-A1 优先权日:1999-03-08 标 题:Combined resin method for high-speed synthesis of combinatorial libraries 发明人:LOU BOLIANG; GHARBAOUI TAWFIK 摘要:A method for high-speed parallel synthesis of combinatorial libraries is disclosed where two or more resins of dissimilar functionality are combined in the same reaction vessel in which a plurality of chemical reactions are carried out to create multiple compounds which are then sequentially and individually cleaved from the different resins under the appropriate cleavage conditions for each resin. As used herein resins are considered different when they exhibit different chemical activity in the presence of cleaving or releasing agents. The resins are different when the individual resins have either dissimilar polymeric backbones or dissimilar linkers or both and thus have a different chemical activity in the presence of a release or cleaving agent from the other resins in the reaction vessel.
专利号:US-6600016-B1 优先权日:1999-08-24 标题:Multifunctionalized solid support resins for synthesis of combinatorial libraries and method for using the same 发明人:CAMPIAN EUGENE; LU BOLIANG; ZHANG JINFANG 权利人:ADVANCED SYNTECH LLC 摘要:Multifunctionalized support resin for the solid phase synthesis of combinatorial libraries is disclosed. The support resin comprises a resin backbone to which is attached a template containing at least two more attachment points which carry mutiple functionalized benzyl-type linkers. Each linker displays differing chemical stability under cleavage conditions so that products can be selectively and sequentially cleaved and separated from the reaction vessel. The linkers are independently different benzyl-type moieties, and each product synthesized on the linkers may have a different chemical structure. The support resin may further comprise an additional linker which is directly attached to the resin backbone. This linker can benzyl-type linkers or other traditional cleavable-linkers. The invention is further directed to a method for the production of mutiple combinatorial libraries in a simultaneous fashion utilizing the above described support resin. The products are selectively cleaved under conditions where only one linker site is cleaved so that the product is individually separated from the reaction vessel.
专利号:US-8987504-B2 优先权日:2010-06-18 标题 :Aminohydroxylation of alkenes 发明人:MEE SIMON PETER HAROLD; LUXENBURGER ANDREAS; HARRIS LAWRENCE DANIEL 权利人:MEE SIMON PETER HAROLD; LUXENBURGER ANDREAS; HARRIS LAWRENCE DANIEL; VICTORIA LINK LTD 摘要:The invention relates to a process for the aminohydroxylation of alkenes using N-oxycarbamate reagents, e.g. N-acyloxycarbamate, N-alkyloxycarbonyloxycarbamate and N-aralkoxycarbonyloxycarbamate reagents. The invention particularly relates to an intermolecular aminohydroxylation reaction that can be carried out in the absence of added base. The invention also relates to novel N-oxycarbamate reagents that are stable crystalline materials. The process of the invention is useful in the synthesis of compounds having a vicinal amino alcohol moiety, such as biologically active compounds.
专利号:US-6528275-B1 优先权日:1996-04-24 标题:Substrates and inhibitors of proteolytic enzymes 发明人:QUIBELL MARTIN; JOHNSON TONY; HART TERANCE 权利人:MEDIVIR UK LTD 摘要:The present invention relates to the field of compounds which are substrates or inhibitors of proteolytic enzymes and to apparatus and methods for identifying substrates or inhibitors for proteolytic enzymes. We have devised a combinatorial method for the rapid indentification of binding motifs which will greatly expedite the synthesis of inhibitors of a variety of proteolytic enzymes such as aspartyl proteases, serine proteases, metallo proteases and cysteinyl proteases.
专利号:US-6608193-B2 优先权日:2001-12-21 标题 :Methods for synthesis of amino-tetrahydroisoquinoline ring compounds 发明人:LIU SONG; RENNELLS WILLIAM MARTIN 权利人:PROCTER & GAMBLE 摘要:Methods of preparing amino-substituted-tetrahydroisoquinoline ring compounds include the steps of providing a support-bound amino-substituted-tetrahydroisoquinoline compound; forming an intermediate by reacting the support-bound amino-substituted-tetrahydroisoquinoline compound with a reagent; and cyclizatively cleaving the support-bound amino-substituted-tetrahydroisoquinoline compound to form the amino-substituted-tetrahydroisoquinoline ring compound.
专利号:US-8147799-B2 优先权日:2007-01-11 标题:Methods and compositions for improved F-18 labeling of proteins, peptides and other molecules 发明人:MCBRIDE WILLIAM J; GOLDENBERG DAVID M 权利人:MCBRIDE WILLIAM J; GOLDENBERG DAVID M; IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen. Exemplary results show that F-18 labeled targetable conjugate peptides are stable in human serum at 37° C. for several hours, sufficient time to perform PET imaging analysis.