其它别名2-(Dicyclohexylphosphino)-3,6-dimethoxy-2'-4'-6'-tri-i-propyl-1,1'-biphenyl, min. BrettPhos; 2-(Dicyclohexylphosphino)3,6-dimethoxy-2′,4′,6′-triisopropyl-1,1′-biphenyl; Dicyclohexyl(2',4',6'-triisopropyl-3,6-diMethoxy-[1,1'-biphenyl]-2-yl)phosphine
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-2024336649-A1 优先权日:2021-06-21 标 题 :Synthesis of covalent protein dimers that can inhibit myc-driven transcription 发明人:LOAS ANDREI; PENTELUTE BRADLEY L; POMPLUN SEBASTIAN; JBARA MUHAMMAD; SCHISSEL CARLY KATHERINE; RODRIQUEZ JACOB JOSHUA LEE; BUCHWALD STEPHEN LEFFLER; BOIJA ANN; KLEIN ISAAC; HAWKEN SUSANA WILSON; LI CHARLES HAN 权利人:MASSACHUSETTS INST TECHNOLOGY; WHITEHEAD INSTITUTE OF BIOMEDICAL RES 摘要:The disclosure relates to covalent protein dimers of MYC, MAX, and Omomyc; pharmaceutical compositions comprising the covalent protein dimers; methods of making the covalent protein dimers; and methods of treating disorders associated with MYC dysregulation (e.g., cancer) with the covalent protein dimers.
专利号:US-2023183246-A1 优先权日:2020-05-19 标题 :Continuous flow sonogashira coupling synthesis method 发明人:THOMPSON DAVID HARLEY; SINTIM HERMAN O; QI QINGQING; BIYANI SHRUTI 权利人:PURDUE RESEARCH FOUNDATION 摘要:The present disclosure relates to a telescoped continuous flow Sonogashira coupling synthesis for some lead compounds to support in vivo studies and pre-clinical evaluation. The application of high throughput tools combined with the telescoped continuous synthesis method can enable an efficient and safe synthesis of compounds of interest involving hazardous coupling reagents such as HATU, while minimizing by-product formation.
专利号:US-2023405565-A1 优先权日:2022-06-21 标 题:Catalyst composition for biaryl synthesis by decarboxylative cross-coupling 发明人:LIM CHERN-HOOI; QIAN GANG; ELDER WILLIAM ZACHARY; RILEY PAIGE; KOLVENBACH ROBIN; WALTER PHILIPP; GOCK MICHAEL 权利人:HERAEUS DEUTSCHLAND GMBH & CO KG; NEW IRIDIUM INC 摘要:The present invention relates to a catalyst composition for synthesis of heteroaromatic biaryls by a light-assisted decarboxylative carbon-carbon cross-coupling reaction, wherein the composition comprises(i) a palladium compound which is selected from a palladium salt or a palladium complex or a mixture thereof,(ii) at least one of the following compounds:a compound of Formula (I)a compound of Formula (II)an iridium complex comprising ligands L1, L2 and L3, wherein the ligands L1, L2 and L3 are selected, independently from each other, from a phenylpyridine and a bipyridine.
专利号:US-2024208926-A1 优先权日:2021-03-24 标题:New process for the synthesis of 5-{5-chloro-2-[(3s)-3-[(morpholin-4-yl)methyl]-3,4-dihydroisoquinoline-2(1h)- carbonyl]phenyl}-1,2-dimethyl-1h-pyrrole-3-carboxylic acid derivatives and its application for the production of pharmaceutical compounds 发明人:PIN FRÉDÉRIC; PETHÖ BÃ?LINT 权利人:SERVIER LAB; NOVARTIS AG 摘要:The present invention relates to a new process for preparing 5-{5-chloro-2-[(38)-3-[(morpholin-4-yl)methyl]-3.4-dihydr oisoquinoline-2(1H)-carbonyl]phenyl}-1,2-dimethyl-1/H-pyrrole-3-carboxylic acid derivatives and its application for the production of pharmaceutical compounds.
专利号:US-2024174698-A1 优先权日:2022-09-23 标题 :Modular synthesis of 1,2-azaborines via ring-opening bn-isostere benzannulation 发明人:DONG GUANGBIN; LYU HAIRONG; CHEN ZHIJIE; WU YIFEI; CHOI SHINYOUNG 权利人:UNIV CHICAGO 摘要:The present disclosure relates generally to 1,2-azaborines and methods of making the same.
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 247. 摘要:Stanforth, S. P., Science of Synthesis Knowledge Updates, (2015) 1, 199. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 78. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 68. 摘要:Littke, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 204.