专利号:US-8829238-B2 优先权日:2011-09-22 标 题:Methods for the synthesis of deuterated acrylate salts 发明人:YANG JUN; BONNESEN PETER V; HONG KUNLUN 权利人:YANG JUN; BONNESEN PETER V; HONG KUNLUN; UT BATTELLE LLC 摘要:A method for synthesizing a deuterated acrylate of the Formula (1), the method comprising: (i) deuterating a propiolate compound of Formula (2) to a methyne-deuterated propiolate compound of Formula (3) in the presence of a base and D 2 O: and (ii) reductively deuterating the methyne-deuterated propiolate compound of Formula (3) in a reaction solvent in the presence of deuterium gas and a palladium-containing catalyst to afford the deuterated acrylate of the Formula (1). The resulting deuterated acrylate compounds, derivatives thereof, and polymers derived therefrom are also described.
专利号:US-2024059678-A1 优先权日:2021-01-18 标 题 :Synthesis Method for Aminopyrimidine FAK Inhibitor Compound 发明人:DU WU; LV HAIBIN; LI YU; KUANG TONGTAO; GENG XI 权利人:HINOVA PHARMACEUTICALS INC 摘要:A synthesis method for an aminopyrimidine FAK inhibitor compound, relating to the field of pharmaceutical synthesis. In the synthesis method, R1 is hydrogen or a carboxylic acid protecting group, R2 is selected from C1ËœC6 alkyl or C1ËœC6 deuterated alkyl, R3 and R4 are each independently selected from hydrogen or deuterium, and R5 is selected from C1ËœC6 alkyl or C1ËœC6 deuterated alkyl. The synthesis method is simple to operate, and has low costs. The product prepared can obtain a high total yield (≥66%) and a high purity (≥99%), and the product yield and purity are superior to those in the prior art (in the prior art, the total yield is about 11%, and the purity is 99%). The synthesis method achieves excellent effects, can also successfully prepare a final product on kilogram scale, and is suitable for industrial production, having a good application prospect.
专利号:US-2024286990-A1 优先权日:2021-06-18 标题:Vinylated keto esters with applicability in signal enhanced magnetic resonance imaging and synthesis thereof 发明人:GLÖGGLER STEFAN; KORCHAK SERGEY; JAGTAP ANIL P; SAUL PHILIP; MOLL DENIS 权利人:MAX PLANCK GESELLSCHAFT 摘要:The present invention relates to a vinyl keto ester and intermediates of its synthesis, wherein the vinyl moiety of the vinyl hydroxy ester and of the intermediates is partly or fully deuterated. Furthermore, the present invention relates to two alternative methods of preparing said vinyl keto ester. The first method is a multi-step approach comprising the steps of providing a carboxylic acid that comprises a geminal diol moiety protected by a photolabile protecting group, vinylating said carboxylic acid using vinyl acetate, and cleaving the protecting group by applying UV light. The second method is a one-step approach of reacting a carboxylic acid that comprises an additional carbonyl moiety with acetylene in the presence of a metal catalyst. In both methods, the compounds used may be fully or partly deuterated.
专利号:US-8952042-B2 优先权日:2009-08-19 标 题 :FXR (NR1H4) binding and activity modulating compounds 发明人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF 权利人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF; PHENEX PHARMACEUTICALS AG 摘要:The present invention relates to compounds of formula (1): n nwhere R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
专利号:US-2013079554-A1 优先权日:2011-09-22 标 题 :Methods for the synthesis of deuterated acrylate salts
专利号:US-8633204-B2 优先权日:2006-09-15 标 题 :4-methylpyridopyrimidinone compounds 发明人:CHENG HENGMIAO; BHUMRALKAR DILIP; DRESS KLAUS RUPRECHT; HOFFMAN JACQUI ELIZABETH; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; LE PHUONG THI QUY; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; PLEWE MICHAEL BRUNO; TRAN KHANH TUAN 权利人:CHENG HENGMIAO; BHUMRALKAR DILIP; DRESS KLAUS RUPRECHT; HOFFMAN JACQUI ELIZABETH; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; LE PHUONG THI QUY; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; PLEWE MICHAEL BRUNO; TRAN KHANH TUAN; PFIZER 摘要:The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), n nand to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-Kα).
参考文献:10.1007/s00216-014-7826-4 摘要:Wensbo Posaric D, Andersson A, Bergquist K, Isaksson A. Differentiation and quantification of synthetic phosphatidylethanol (PEth) homologues by 1H- and 13C-NMR in polar organic solvents. Analytical and Bioanalytical Chemistry. 2014 May 28;406(19):4735–44. doi: 10.1007/s00216-014-7826-4. 参考文献:10.1007/s11095-009-0038-5 摘要:Desai KGH, Olsen KF, Mallery SR, Stoner GD, Schwendeman SP. Formulation and In Vitro-In Vivo Evaluation of Black Raspberry Extract-Loaded PLGA/PLA Injectable Millicylindrical Implants for Sustained Delivery of Chemopreventive Anthocyanins. Pharmaceutical Research. 2010 Feb 11;27(4):628–43. doi: 10.1007/s11095-009-0038-5.