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-2025236633-A1 优先权日:2022-03-28 标 题:Synthesis of isomerically pure polyol-based phosphoramidites 发明人:BANASIK BRENT; DIAZ CORRAL JULIAN ANDRES; JACOBS AARON; JUD LUKAS; KUCHELMEISTER HANNES; NBAVI MELUD; PFAFFENEDER TONI; SIMONYIOVA SONA; TABONE JOHN C; THUER WILMA 权利人:ROCHE SEQUENCING SOLUTIONS INC 摘要:The present disclosure relates to a process for the regiochemically and enantiomerically controlled synthesis of phosphoramidite-containing monomers, and to intermediate products of this process. In some embodiments, the phosphoramidite-containing monomers or their precursors are regioisomerically and/or enantiomerically pure and may be polymerized into polymers or copolymers.
专利号:US-2013012706-A1 优先权日:2010-03-01 标 题 :Methods and Intermediates for the Synthesis of 4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazines 发明人:HUMMERSONE MARC GEOFFERY; COUSIN DAVID 权利人:PHARMINOX LTD; HUMMERSONE MARC GEOFFERY; COUSIN DAVID 摘要:The present invention provides a compound of general formula (II), or a salt or solvate thereof: n n n n n n n n n n n n wherein n A is independently -A 1 , -A 2 , -A 3 , -A 4 , -A 5 , -A 6 , or -A 7 , wherein:n -A 1 is independently C 5-12 heteroaryl, and is optionally substituted; -A 2 is independently thioamido or substituted thioamido; -A 3 is independently imidamido, substituted imidamido, N-hydroxyimidamido, or substituted N-hydroxyimidamido; -A 4 is independently hydroxamic acid or hydroxamate; -A 5 is independently carboxamide or substituted carboxamide; -A 6 is independently aliphatic C 2-6 alkenyl, and is optionally substituted; and -A 7 is independently carboxy or C 1-4 alkyl-carboxylate;n nand its use in the synthesis of temozolomide and analogues thereof.
专利号:US-2025091989-A1 优先权日:2023-09-19 标 题 :Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:WO-2022238500-A1 优先权日:2021-05-12 标题 :Radiosynthesis of [18f] talazoparib 发明人:BOWDEN GREGORY DAVID; MAURER ANDREAS; STOTZ SOPHIE; KINZLER PAUL JOHANNES OSKAR MARIA; LAEMMERHOFER MICHAEL; ZENDER LARS; PICHLER BERND 权利人:UNIV TUEBINGEN MEDIZINISCHE FAKULTAET 摘要:The present invention relates to the synthesis of Poly (ADP ribose) polymerase (PARP) inhibitors and particularly to the radiosynthesis of PARP 1 inhibitors, more particularly to the synthesis of [18F] talazoparib.
专利号:US-2025197439-A1 优先权日:2022-03-18 标 题:Decarboxylative acetoxylation using mn(ii) or mn(iii) reagent for synthesis of 4'-acetoxy-nucleoside and use thereof for synthesis of corresponding 4'-(dimethoxyphosphoryl)methoxy-nucleotide 发明人:VAGLE KURT EDRIC; BHADURI SAYANTAN; YANG GUOHAN 权利人:DICERNA PHARMACEUTICALS INC 摘要:The present invention relates to the preparation of nucleic acids, nucleosides, nucleotides, and analogues thereof useful as potent and stable RNA interference agents. The present invention provides improved yields and avoids the use of lead tetraacetate for decarboxylative acetylation which decreases the overall cost of production by removing the need for lead remediation and offers a significant reduction in the environmental costs in production.
摘要:Wong, Y.-S., Science of Synthesis, (2009) 46, 596. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 340. 摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 286. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 215. 摘要:Sapeta, K.; Kerr, M. A., Science of Synthesis Knowledge Updates, (2011) 1, 57.