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-11066395-B2 优先权日:2016-09-30 标题:Dimethylaminoethanol salt of a GLP-1 receptor modulator 发明人:VIDAL EPHRAIM; BAKALE ROGER; TURNBULL PHILIP; MOSER DAVID; ROBBINS ANDREW; GRANT CRAIG 权利人:RECEPTOS LLC 摘要:Crystalline 2-hydroxy-N,N-dimethylethanaminium 1-(2-(5-(tert-butyl)-thiophene-2-carboxamido)-3-(4-(5-(4′-ethyl-[1,1′-bi(cyclohexan)]-3-en-4-yl)pyrimidin-2-yl)phenyl)propanoyl)azetidine-3-carboxylate salt, and methods related to synthesis and therapeutic use of the same.
专利号:JP-2012528861-A 优先权日:2009-06-03 标 题 :Stereoselective synthesis of specific trifluoromethyl substituted alcohols.