专利号:US-2004138469-A1 优先权日:2002-12-23 标 题 :Process for the synthesis of torsemide, in particular of pure and stable form II 发明人:LUSSANA MASSIMILIANO; RAINONI MAURO; GAMBUZZA FILIPPO 权利人:COSMA S P A 摘要:The present invention relates to a new process for the synthesis of torsemide, in particular of pure and stable form II, which comprises direct synthesis of torsemide from 4-(3-methylphenylamino)-3-pyridine-sulphonamide. The new process envisages fewer steps than the processes described in the prior art, with improved yields and good quality from the chemical and preferably polymorphous points of view.
专利号:US-12338202-B2 优先权日:2021-09-10 标 题 :One pot synthesis of urea (meth)acrylates 发明人:BESTGEN SEBASTIAN; BEYER SILVIA 权利人:EVONIK OPERATIONS GMBH 摘要:A one-pot synthesis of polymerizable and acyclic urea (meth)acrylates, preferably mono(meth)acrylates, can be performed via in-situ synthesis of urea alcohols or amines followed by direct reaction with a (meth)acrylate reactive diluent. The urea alcohol/amine is obtained from isocyanates and alcohols, amines, or hydroxyamines. Subsequently, the reaction with the (meth)acrylate reactive diluent takes place and the urea (meth)acrylate is directly obtained either in solution with the reactive diluent, or as a pure material after removal of the reactive diluent.
专利号:US-5696290-A 优先权日:1994-09-12 标 题:Synthesis of penta-substituted guanidines 发明人:RUETTIMANN KENNETH W; MCGHEE WILLIAM D; SOLODAR A JOHN 权利人:MONSANTO CO 摘要:The present invention is the novel synthesis of sterically hindered penta-substituted guanidines by a process in which (1a) an isocyanate is reacted first with a di-substituted amine or (1b) a urea is reacted with two moles of a mono-substituted amine to form a tri-substituted urea followed by (2) treatment of the tri-substituted urea with an activating agent before reacting with a second di-substituted amine in the presence of a base.
专利号:US-11655255-B2 优先权日:2022-10-17 标题 :Method for catalytic asymmetric synthesis of phosphorus-stereogenic (P-stereogenic) nucleoside derivative and catalyst used therein 发明人:ZHANG WANBIN; WANG MO; ZHANG LU; HUO XIAOHONG; ZHANG ZHENFENG; YUAN QIANJIA; CHEN JIANZHONG 权利人:SPH NO 1 BIOCHEMICAL & PHARMACEUTICAL CO LTD; UNIV SHANGHAI JIAOTONG 摘要:A method for catalytic asymmetric synthesis of a phosphorus-stereogenic (P-stereogenic) nucleoside derivative of formula (3) and a catalyst used therein. The P-stereogenic nucleoside derivative (3) can be hydrolyzed to obtain remdesivir. Specifically, a nucleoside and phosphoryl chloride are subjected to asymmetric reaction under the catalysis of a chiral bicyclic imidazole catalyst in the presence of a base to produce the P-stereogenic nucleoside derivative of formula (3)
专利号:US-6919382-B2 优先权日:2000-08-31 标 题 :Preparation and uses of conjugated solid supports for boronic acids 发明人:HALL DENNIS G 权利人:UNIV ALBERTA 摘要:The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.
专利号:US-3781324-A 优先权日:1969-11-03 标 题:Certain 6-trifluoromethylcytosines and thiocytosines,their synthesis,and their use in the synthesis of uracils and thiouracils 发明人:LUTZ A 权利人:AMERICAN CYANAMID CO 摘要:3-AMINO-2-SUBSTITUTED - 4,4,4 - TRIFLUORO-2-BUTENENITRILES ARE REACTED WITH ISOCYANATES OR ISOTHIOCYANATES IN THE PRESENCE OF AN INERT SOLVENT AND FROM 0.75 TO ABOUT 1.0 MOLE EQUIVALENTS OF STRONG BASE PER MOLE OF BUTENENITRILE TO PRODUCE THE NOVEL UREIDO BUTENENITRILES OF THE FORMULA: CF3-C(-NH-C(=X)-NH-R)=C(-HALO)-CN WHEREIN R IS ALKYL, ALKENYL, PHENYL, BENZYL AND SUBSTITUTED DERIVATIVES THEREOF AND X IS SULFUR OR OXYGEN. THE UREIDO BUTENENITRILE ARE TREATED WITH ADDITIONAL BASE TO PRODUCE NOVEL CYCLIC CYTOSINES OF THE FORMULA: 6-CF3,5-HALO,4-(HN=),3-R,2-(X=)-1,2,3,4-TETRAHYDRO- PYRIMIDINE WHEREIN R AND X ARE AS DEFINED ABOVE. THE CYTOSINES CAN BE PRODUCED DIRECTLY BY TREATING 3-AMINO-2-SUBSTITUTED4,4,4-TRIFLUORO-2-BUTENENITRILE WITH AT LEAST 1.0 MOLE EQUIVALENT OF BASE. THE NOVEL COMPOUNDS ARE USEFUL INTERMEDIATES IN THE PREPARATION OF HERBICIDAL URACILS AND THIOURACILS.