专利号:WO-2012173572-A1 优先权日:2011-06-10 标 题 :Stereoselective synthesis of highly substituted enamides 发明人:PARK CHEOL-MIN; LIU YU 权利人:UNIV NANYANG TECH; PARK CHEOL-MIN; LIU YU 摘要:The disclosure provides new methods for the oxidative Heck cross-coupling reaction with electron-rich alkenes such as substituted β-amidoacrylate and other related substituted enamides. Previously, functionalization of enamides under Heck conditions has been limited to those with unsubstituted vinyl groups. By tuning the reaction parameters that allow for the balance between stability and reactivity of the reactants, the oxidative Heck cross-coupling reaction now provides highly substituted enamides in good to excellent yields. (II) (III) (I)·
专利号:US-9243004-B2 优先权日:2011-07-22 标题 :Synthesis of boronic esters and boronic acids using grignard reagents 发明人:CLARY JACOB W; SINGARAM BAKTHAN 权利人:CLARY JACOB W; SINGARAM BAKTHAN; UNIV CALIFORNIA 摘要:Boronic esters and boronic acids are synthesized at ambient temperature in an ethereal solvent by the reaction of Grignard reagents with a boron-containing substrate. The boron-containing substrate may be a boronic ester such as pinacolborane, neopentylglycolborane, or a dialkylaminoborane compound such as diisopropylaminoborane. The Grignard reagents may be pre-formed or generated from an alkyl, alkenyl, aryl, arylalkyl, heteroaryl, vinyl, or allyl halide compound and Mg 0 . When the boron-containing substrate is a boronic ester, the reactions generally proceed at room temperature without added base in about 1 to 3 hours to form a boronic ester compound. When the boron-containing substrate is a dialkylaminoborane compound, the reactions generally proceed to completion at 0° C. in about 1 hour to form a boronic acid compound.
专利号:US-9708336-B2 优先权日:2014-01-22 标题 :Metallo-beta-lactamase inhibitors 发明人:MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
专利号:US-7122694-B2 优先权日:1998-11-06 标 题 :Hydroboronation process 发明人:MARCUCCIO SEBASTIAN MARIO; RODOPOULOS MARY; WEIGOLD HELMUT 权利人:BORON MOLECULAR PTY LTD 摘要:The invention relates to processes for the synthesis of aryl or alkene borates which comprises reacting: (i) an olefinic compound having a halogen or halogen-like substituent in a vinylic substitution position, or (ii) an aromatic ring having a halogen or halogen-like substituent in a ring substitution position, with a disubstituted monohydroborane in the presence of a Group 8-11 metal catalyst. The invention also relates to the use of these borates in coupling reactions. The invention further relates to certain disubstituted monohydroboranes and aryl or alkene borates.
专利号:US-2015119580-A1 优先权日:2011-07-22 标 题 :Synthesis of boronic esters and boronic acids using grignard reagents
专利号:WO-2013016185-A1 优先权日:2011-07-22 标 题 :Synthesis of boronic esters and boronic acids using grignard reagents
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