专利号:US-7452994-B2 优先权日:2001-09-12 标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 发明人:MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN 权利人:ANORMED INC 摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.
专利号:US-2023174567-A1 优先权日:2020-05-22 标题:Synthesis of fluorinated nucleotides 发明人:ARMIGER TRAVIS; BELYK KEVIN M; BENKOVICS TAMAS; CHUNG CHEOL K; JI CHEN YINING; JOHNSON HEATHER CLAIRE; KLAPARS ARTIS; LIU ZHIJIAN; LIU ZHUQING; MOORE JEFFREY C; NEEL ANDREW J; PENG FENG; RUMMELT STEPHAN M; SALEHI MARZUARANI NASTARAN; SHERRY BENJAMIN D; SONG ZHIGUO JAKE; TURNBULL BEN WILLIAM HULME; WANG LU; XU FENG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3′-fluoro-thio-guanosine monophosphate or 3′-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. (I)
专利号:US-2020079715-A1 优先权日:2018-09-06 标题 :2-position modification for synthesis of resorcinol scaffolding 发明人:DAVIS ROBERT; BLACK JACOB; SMELTZER THOMAS; COLVIN SEAN 权利人:CANOPY HOLDINGS LLC 摘要:A resorcinol with modifications at the 2-position is provided. The reactant resorcinol may have a variety of functional groups at each of the 1, 3, and 5 position such as a hydroxide, a lower alkyl group, a phenyl, a substituted phenyl, a lower alkenyl, or a lower alkynyl sp 2 carbon group (e.g., substituted phenyl, vinyl), sp (e.g., alkyne), hydrogen. The resorcinol is modified at the 2-position with a nucleophile or an electrophile. The resulting resorcinol may serve as a stable intermediate for the synthesis of cannabinoid or cannabinoid derivatives.
专利号:US-8785656-B2 优先权日:2012-02-16 标 题:Telescoping synthesis of 5-amino-4-nitroso-1-alkyl-1H-pyrazole salt 发明人:GEIBEL WOLFRAM; WEBER INGO; OSAN ARMIN; SPECKBACHER MARKUS 权利人:PROCTER & GAMBLE 摘要:A telescoping synthesis of 5-amino-4-nitroso-1-alkyl-1H-pyrazole salt derivatives of formula (I), the compound (I) itself, and its use as an intermediate in the fabrication of 1-alkyl-4,5-diaminopyrazole salts of general formula (IX). The compounds of formula (IX) can be used as precursor dyes in oxidative hair dye compositions. n n n n n n n n n n R is a mono- or poly-substituted or unsubstituted, straight or branched, saturated or mono- or poly-unsaturated, alkyl group. HZ and HZ′ are organic or mineral acids.
专利号:US-9475780-B2 优先权日:2011-07-20 标 题 :Process for the synthesis of cyclic alkylene ureas 发明人:GUPTA RAM; KOBYLANSKA IRINA; TREASURER URVEE; FLOOD LAWRENCE 权利人:GUPTA RAM; KOBYLANSKA IRINA; TREASURER URVEE; FLOOD LAWRENCE; ALLNEX IP S AR L 摘要:The invention relates to a process for the synthesis of cyclic alkylene ureas comprising reacting in the presence of a basic catalyst, a difunctional amine A having two primary amino groups, and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA, wherein the ratio of the amount of substance Ji(—NH2) of primary amino groups —NH2 in the difunctional amine A to the sum M(C) of the amount of substance n(CD) of carbonate groups of a dialkyl carbonate CD and the amount of substance n(CA) of carbonate groups in an alkylene carbonate CA, is at least more than 2, and to the product obtained by this process.
专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).