专利号:US-2013267680-A1 优先权日:2010-09-15 标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof 发明人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL 权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST 摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.
专利号:US-12162849-B2 优先权日:2018-12-21 标题 :Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or of the methyl-d3 deuterated form thereof 发明人:HOVEYDA HAMID; DUTHEUIL GUILLAUME 权利人:OGEDA SA 摘要:The present invention relates to a method of synthesis of compound (I), wherein R1 represents methyl or methyl-d3, thus corresponding to 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or to the methyl-d3 deuterated form thereof. These compounds are useful as key intermediates in the synthesis of pharmaceutical compounds, especially fezolinetant and deuterated fezolinetant.
专利号:US-3956184-A 优先权日:1974-04-24 标题:Method of preparing silver catalyst for synthesis of formaldehyde by oxidizing methyl alcohol 发明人:KRUGLIKOV ANATOLY ABRAMOVICH; YAKOVENKO ZEMFIRA IVANOVNA; ROZNINA MARINA IVANOVNA; ROGACHEVA ANNA MALOFEEVNA; BELOUSOV GERMAN IVANOVICH 权利人:KRUGLIKOV ANATOLY ABRAMOVICH; YAKOVENKO ZEMFIRA IVANOVNA; ROZNINA MARINA IVANOVNA; ROGACHEVA ANNA MALOFEEVNA; BELOUSOV GERMAN IVANOVICH 摘要:The method of preparing a silver catalyst for synthesis of formaldehyde by oxidizing methyl alcohol which consists in that a carrier is impregnated with an aqueous or an aqueous-alcohol solution containing complex ions of silver having the general formula [Ag(X) n ] + or [Ag(Y) 2 ] - , where X is ammonia, ethylenediamine, triethylenetetramine or triaminotriethylamine, Y is a thiocyanate, cyanide, acetate, or hydroxyl ion, and n is 1 or 2. The impregnated carrier is processed, at a temperature of from 10° - 100°C, with a reducing agent taken in the quantity sufficient to reduce the silver completely from said ion. The thus-prepared catalyst is dried at a temperature of from 80° to 400°C. It is recommended that the catalyst be washed with water before drying. The thus-prepared catalyst has a highly developed active surface with a small content of silver (the specific surface of the catalyst is 0.7 - 7 square meters per gram, with the metal silver content of the catalyst being from 5 - 10 per cent by weight). The catalyst is highly active and has good selectivity in the process of formaldehyde synthesis from methyl alcohol. The yield of formaldehyde with the proposed catalyst is from 75 - 80 per cent, calculating with reference to the passed methyl alcohol, with the selectivity of the process being from 89 - 95 per cent.
专利号:US-11292775-B2 优先权日:2017-12-21 标 题 :Efficient process for the synthesis of 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazole-3-thione(prothioconazole) and its intermediates 发明人:KADAM SUBHASH RAJARAM; JANI NILESH; SHINDE RAVINDRA; SHAH KENAL V; SHAH BHAVESH V; GUJRAL AJIT SINGH; BYREGOWDA GANGANARASAIAH; SIVAIAH GANADI; PAWAR JIVAN DHANRAJ; PATI HARI NARAYAN 权利人:GSP Crop Science Pvt Ltd 摘要:The present invention relates to an improved and efficient process for the synthesis of 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazole-3-thione, compound of formula (I) (Prothioconazole). The present invention more particularly relates to an improved process for manufacturing of 2-(1-chloro-cycloprop-1-yl)-3-(2-chloro phenyl)-2-hydroxy propyl-1-hydrazine (compound of formula III) and 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-1,2,4-triazolidine-3-thione (compound of formula II) which are mainly used for synthesis of Prothioconazole which is knows as an active compound with microbicidal fungicidal properties.
专利号:US-6159673-A 优先权日:1996-07-17 标 题:Oxonol compound, light-sensitive material and process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which Z is an atomic group that forms a cyclic amide ring; each of W1 and W2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.
专利号:US-12281398-B2 优先权日:2022-02-07 标题:Microfluidic process for the general electrochemical synthesis of geminal dipseudohalide or halide-pseudohalide compounds 发明人:SCHROER THORSTEN G; LECROY GREGORY E; AGUILA MIGUEL; RODRIGUEZ MAYRA P; DOWNARD TYLER J; MACLEOD BRIANNA L 权利人:US GOV AIR FORCE; US AIR FORCE 摘要:A process for the microfluidic electrochemical synthesis of geminal dipseudohalide or halide-pseudohalide compounds comprising the steps ofpumping a solution comprising a compound of Formula Iinto a microfluidic electrochemical reactor in the presence of a base, one of a halide or pseudohalide salt (MY), and a mediator;applying an electrical current through the microfluidic electrochemical reactor; andperforming oxidative addition to create a geminal dipseudohalide or halide-pseudohalide compound of the general Formula II
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合成参考文献
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