专利号:US-11858901-B2 优先权日:2019-10-30 标 题:3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6 trifluoromethyl benzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, process for its preparation, and its use in the synthesis of elagolix 发明人:BALLETTE ROBERTO; JIMÉNEZ ALONSO OSCAR; GARCÃ?A GARCÃ?A ELENA; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.
专利号:US-7250510-B2 优先权日:2005-08-24 标 题:Transition metal complexes of N-heterocyclic carbenes, method of preparation and use in transition metal catalyzed organic transformations 发明人:ORGAN MICHAEL G; O'BRIEN CHRISTOPHER J; KANTCHEV ASSAM ERIC B 权利人:TOTAL SYNTHESIS LTD 摘要:The present invention relates to catalysts of transition metal complexes of N-heterocyclic carbenes, their methods of preparation and their use in chemical synthesis. The synthesis, ease-of-use, and activity of the compounds of the present invention are substantial improvements over in situ catalyst generation. Further, the transition metal complexes of N-heterocyclic carbenes of the present invention may be used as precatalysts in metal-catalyzed cross-coupling reactions.
专利号:US-11578040-B2 优先权日:2016-09-30 标题 :[5]Helicene derivatives as molecular reporters for diagnostic applications and methods of synthesis therefor 发明人:SOOKSIMUANG THANASAT; KAROONUTHAISIRI NITSARA; CHARLERMROJ RATTHAPHOL; SAHASITHIWAT SOMBOON; PANCHAN WARAPORN; MAKORNWATTANA MANLIKA; PHUENGWAS SUDTIDA; KANGKAEW LAONGDAO 权利人:NATIONAL SCIENCE AND TECH DEVELOPMENT AGENCY 摘要:The present invention provides the methods of synthesis of [5]helicene compounds and the use of the said compounds conjugating with biomolecules to work as molecular reporter for diagnostic. The compounds in the present invention have the chemical structure illustrated in the formula (1): wherein G is a connecting group composes of 2 carbon atoms selected from the group consisting of ethane and ethylene; A is a separated or connected group selected from the group consisting of cyano and imide; D1 is selected from the group consisting of oxyalkanoic acid, oxyalkanal and oxyalkanesulfonate; and D2 has structure selected from the group consisting of hydroxyl, oxyalkanoic acid, oxyalkanal, alkyl oxyalkanoate, oxyalkanol and oxyalkanesulfonate. The compounds in the present invention compose of aromatic [5]helicene core comprising long it-conjugating system. The said compounds contain functional groups which able to link with biomolecules and they are soluble in water or other solvents that used in binding process with biomolecules. Moreover, owing to having proper chemical structure, the compounds in the present invention exhibit good fluorescent emission in wavelength of 425-675 nm. When the said compounds connected with biomolecules, the biomolecules give good fluorescence and can be detected under ultraviolet radiation.
专利号:WO-2013057186-A1 优先权日:2011-10-19 标题 :Photolabile linker for the synthesis of hydroxamic acids 发明人:NIELSEN THOMAS E; QVORTRUP KATRINE 权利人:UNIV DANMARKS TEKNISKE 摘要:The present invention relates to a photolabile hydroxamate linker based on the o - nitroveratryl group and its application for multistep solid-phase synthesis and controlled photolytic release of hydroxamic acids. The invention provides a method for producing a solid support comprising a hydroxylamine - functionalized photolabile linker, and the so produced hydroxylamine - functionalized photolabile solid support. The invention further provides a method for synthesizing a one-bead-one compound library of hydroxamic acid derivatives on a photolabile linker, as well as a method for screening a library of hydroxamic acid derivatives.
专利号:WO-9939207-A1 优先权日:1998-01-29 标题:Acid cleavable phenoxyalkyl linker for combinatorial synthesis 发明人:LI GE; HE ZHEN MIN 权利人:PHARMACOPEIA INC 摘要:A substrate for solid phase synthesis of formula (I) is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of formula (II) wherein n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; R1 is lower alkyl or phenyl; R2 is lower alkyl or phenyl; and R3 is lower alkyl, phenyl or lower alkoxy.
专利号:US-9850275-B2 优先权日:2013-09-11 标 题 :Photolabile linker for the solid-phase synthesis of hydrazides and pyranopyrazoles 发明人:NIELSEN THOMAS E; QVORTRUP KATRINE 权利人:UNIV DANMARKS TEKNISKE 摘要:The photolabile hydrazine linker of the present invention is based on the o-nitro-veratryl group, which is capable of releasing hydrazide derivatives upon UV irradiation. The linker allows for a new solid-phase peptide synthesis (SPPS) strategy which is fully orthogonal to the most commonly used protecting groups and chemical methods in SPPS and shows excellent compatibility with peptide composition, notably the 20 naturally occurring α-amino acid residues (even in their side-chain protected form) are accepted in the C-terminal of the peptide hydrazides. Furthermore, the linker unit can be applied to synthesize combinatorial libraries of biological interesting heterocyclic compounds, such as pyranopyrazoles.
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合成参考文献
参考文献:10.1107/s1600536811011871 摘要:Fu CY, Liu YH, Zhou ZL, Tang H. 4,4'-[4,4'-Sulfonyl-bis-(p-phenyl-ene-oxy)]dibutanoic acid. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1048.