专利号:US-2004058888-A1 优先权日:2000-01-13 标题:Methods for synthesis of alpha-d-gal (1~>3) gal-containing oligosaccharides 发明人:BORNAGHI LAURENT; DEKANY GYULA; DRINNAN NICHOLAS BARRY; PAPAGEORGIOU JOHN; WEST MICHAEL LEO 摘要:This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R 3 is methoxy or methyl; R 1 is H, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R 2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4 -chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.
专利号:US-9012625-B2 优先权日:2009-04-07 标 题 :Method for the synthesis of a trisaccharide 发明人:DÉKANY GYULA; Ã?GOSTON KÃ?ROLY; BAJZA ISTVAN; BOUTET JULIEN; BØJSTRUP MARIE; FANEFJORD METTE; PÉREZ FIGUEROA IGNACIO; HEDEROS MARKUS; HORVATH FERENC; KOVÃ?CS-PÉNZES PIROSKA; KRÖGER LARS; OLSSON JOHAN; RÖHRIG CHRISTOPH; SCHROVEN ANDREAS; VRASIDAS IOANNIS 权利人:DÉKANY GYULA; Ã?GOSTON KÃ?ROLY; BAJZA ISTVAN; BOUTET JULIEN; BØJSTRUP MARIE; FANEFJORD METTE; PÉREZ FIGUEROA IGNACIO; HEDEROS MARKUS; HORVATH FERENC; KOVÃ?CS-PÉNZES PIROSKA; KRÖGER LARS; OLSSON JOHAN; RÖHRIG CHRISTOPH; SCHROVEN ANDREAS; VRASIDAS IOANNIS; GLYCOM AS 摘要:The present invention relates to an improved synthesis of a trisaccharide of the formula (1), novel intermediates used in the synthesis and the preparation of the intermediates.
专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:WO-2021038581-A1 优先权日:2019-08-30 标题 :A one step synthesis of 2-substituted benzo[b]thiophenes 发明人:SEKAR GOVINDASAMY; POONGUZHALI ELAMVAZHUTHI 权利人:INDIAN INST TECH MADRAS 摘要:The invention pertains to a one step synthesis of 2-substituted benzo[ b ]thiophene of general formula wherein the synthesis of 2-substituted benzo[ b ]thiophenes is by reacting the starting materials substituted or unsubstituted 2-halogenobenzaldehyde and substituted or unsubstituted acetyl/phenacyl bromide with a catalyst, a sulphur source and phase transfer catalyst in an aqueous medium with atmospheric air and at temperature in the range of 25°C-30°C.
专利号:US-11542269-B2 优先权日:2018-01-03 标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHOI HYEONG-WOOK; FANG FRANCIS G 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
专利号:US-10913749-B2 优先权日:2015-05-07 标 题 :Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
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合成参考文献
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