专利号:US-12240835-B2 优先权日:2018-09-18 标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity 发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI 权利人:TERNS PHARMACEUTICALS INC 摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.
专利号:US-8629288-B2 优先权日:2008-02-25 标题:Method for the regioselective synthesis of 1-alky1-3-haloalkyl-pyrazole-4-carboxylic acid derivatives 发明人:PAZENOK SERGII; LUI NORBERT; HEINRICH JENS-DIETMAR; WOLLNER THOMAS 权利人:PAZENOK SERGII; LUI NORBERT; HEINRICH JENS-DIETMAR; WOLLNER THOMAS; BAYER IP GMBH 摘要:The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives, and to the hydrazones formed as intermediates in the process.
专利号:US-12435086-B2 优先权日:2020-04-29 标题:Synthesis of heterocyclic compounds 发明人:LIN JACK; WALTERS JASON 权利人:PLEXXIKON INC 摘要:Provided herein are intermediates and processes useful for facile synthesis of compounds of Formula 2:wherein R1 is C(O)R2; R2 is alkyl optionally substituted with 1-5 halogens; G is phenyl or a 5-6 membered heteroaryl optionally substituted with 1-2 R3; and each R3 is independently C1-C6 alkyl, CN, C1-C6 alkyl-CN, 3-6 membered cycloalkyl, or 4-6 membered heterocycloalkyl.
专利号:US-2023357257-A1 优先权日:2020-12-28 标 题 :Novel process for the synthesis of noroxymorphone from morphine 发明人:GORBACHEV DMITRY; LAM HON WAI; SAXENA AAKARSH; SAXENA NAVIN SATYAPAL 权利人:NAVIN SAXENA RESEARCH & TECH PVT LTD 摘要:The present invention relates to a novel, efficient, pot- and atom-economical, and industrially applicable process for converting morphine to noroxymorphone using reagents and solvents of lesser toxicity and lower cost with respect to those used in the prior art.
专利号:US-4255594-A 优先权日:1979-09-18 标题 :Hydrogenation of halogen-containing carboxylic anhydrides 发明人:NOVOTNY MIROSLAV 权利人:ALLIED CHEM 摘要:A process is described for the heterogeneous hydrogenation of haloalkyl, halocycloalkyl or haloaryl carboxylic anhydrides to the corresponding primary alcohols. In the haloalkyl or halocycloalkyl carboxylic anhydrides at least one halogen is in the alpha-position relative to the carboxylic anhydride grouping. The hydrogenation can be carried out in the liquid or vapor phase in the presence of a supported or unsupported catalyst comprising a member of the group consisting of rhodium, iridium, metal oxides thereof, or mixtures thereof. In the liquid phase, the hydrogenation can be carried out batchwise under mild conditions of temperature and pressure, preferably at about 50°-150° C. and about 5-15 atmospheres, in an atmosphere containing hydrogen gas. A preferred embodiment is the hydrogenation of trifluoroacetic anhydride in the liquid phase to 2,2,2-trifluoroethanol, said alcohol being useful as an intermediate in the synthesis of the anesthetic, isoflurane, CF 3 CHClOCHF 2 .
专利号:US-7884128-B2 优先权日:2005-10-13 标题:Process for total synthesis of pladienolide B and pladienolide D 发明人:KANADA REGINA MIKIE; ITO DAISUKE; SAKAI TAKASHI; ASAI NAOKI; KOTAKE YOSHIHIKO; NIIJIMA JUN 权利人:EISAI R&D MAN CO LTD 摘要:Process for producing compound of Formula: n nwherein P 2 , P 3 and R 2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7):n n nwherein P 3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8):n n nwherein P 2 means a protecting group for hydroxy group; and R 2 means a phenyl group which may be substituted, in the presence of a base.
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 159. 摘要:Wu, S.; Song, H.; Hu, M., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 113. 摘要:Wu, S.; Song, H.; Hu, M., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 39.