专利号:US-10544177-B2 优先权日:2016-12-06 标 题:Chiral dihydrobenzooxaphosphole ligands and synthesis thereof 发明人:DESROSIERS JEAN-NICOLAS; FANDRICK DANIEL ROBERT; HADDAD NIZAR; LI GUISHENG; PATEL NITINCHANDRA D; QU BO; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; SIEBER JOSHUA DANIEL; TAN ZHULIN; WANG XIAO-JUN; YEE NATHAN K; ZHANG LI; ZHANG YONGDA 权利人:BOEHRINGER INGELHEIM INT 摘要:This invention relates to novel phosphorous ligands useful for organic transformations. Methods of making and using the ligands in organic synthesis are described. The invention also relates to processes for preparing the novel ligands.
专利号:US-9006491-B2 优先权日:2009-10-22 标题 :Structure and method for synthesizing and using dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine and its tetrafluoroborate 发明人:MA SHENGMING; LÜ BO; FU CHUNLING 权利人:MA SHENGMING; LÜ BO; FU CHUNLING; UNIV ZHEJIANG 摘要:The current invention relates to the structure, synthesis of dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate, as well as its applications in the palladium catalyzed carbon-chlorine bond activation for Suzuki coupling reactions and carbon-nitrogen bond formation reactions. The dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate could coordinate with the palladium catalyst to activate the inert carbon-chlorine bond highly selectively and catalyze Suzuki coupling reaction with arylboronic acid or carbon-nitrogen bond formation reaction with organic amines. The current invention uses only one step to synthesize dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine and its tetrafluoroborate is stable in the air. Compared with known synthetic routes of ligands used in activating carbon-chlorine bonds, the method of current invention is short, easy to operate. Moreover, with this type of ligands, the Suzuki coupling products of optically active chlorolactones and arylboronic acids would maintain their configuration and optical purity.
专利号:US-7671085-B2 优先权日:2002-11-15 标 题 :Non-steroidal farnesoid X receptor modulators and methods for the use thereof 发明人:DOWNES MICHAEL R; EVANS RONALD M 权利人:SALK INST FOR BIOLOGICAL STUDI 摘要:The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.
专利号:CN-117700459-B 优先权日:2023-12-25 标题 :Synthesis and application of a type of benzo five-membered C-P ring skeleton monophosphine ligand
专利号:CN-117700459-A 优先权日:2023-12-25 标 题:Synthesis method and application of a type of benzo five-membered C-P ring skeleton monophosphine ligand
专利号:US-11794180-B2 优先权日:2015-10-29 标 题 :Tri-(adamantyl)phosphines and applications thereof 发明人:CARROW BRAD P; CHEN LIYE 权利人:UNIV PRINCETON 摘要:In one aspect, phosphine compounds comprising three adamantyl moieties (PAd3) and associated synthetic routes are described herein. Each adamantyl moiety may be the same or different. For example, each adamantyl moiety (Ad) attached to the phosphorus atom can be independently selected from the group consisting of adamantane, diamantane, triamantane and derivatives thereof. Transition metal complexes comprising PAd3 ligands are also provided for catalytic synthesis including catalytic cross-coupling reactions.