专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-9567293-B2 优先权日:2013-02-08 标题 :Combined synthesis of a nitrile-ester/acid and of a diester/diacid 发明人:DUBOIS JEAN-LUC; COUTURIER JEAN-LUC; BRANDHORST MARKUS 权利人:ARKEMA FRANCE 摘要:A method for the combined synthesis of a mono-unsaturated nitrile-ester(acid) and of a bi-functional carbonyl compound, wherein it includes a step including the cross metathesis mc1 of an unsaturated fatty acid/ester compound with an unsaturated nitrile compound, in which mc1 is performed with partial conversion such as to obtain and recover, separately, at least the following products: a mono-unsaturated nitrile-ester/acid and a symmetrical compound, diester or diacid respectively including a double bond located in the middle of the molecular chain of compound, and subsequently a step including the oxidation cleavage cp2 of the double bond of compound, such as to form a single type of carbonyl compound having formula R2-(CH2)n-COR′, in which R′ is H or OH, depending on the operating conditions selected for the oxidation cleavage cp2. Also, the production of monomers for the polymer industry.
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.
专利号:US-3635977-A 优先权日:1969-11-03 标 题 :Certain 6-trifluoromethylcytosines and thiocytosines their synthesis and their use in the synthesis of uracisls and thiouracil 发明人:LUTZ ALBERT WILLIAM 权利人:AMERICAN CYANAMID CO 摘要:3 - AMINO - 2 - SUBSTITUTED - 4,4,4 - TRIFLUORO - 2 - BUTENENITRILES ARE REACTED WITH ISCYANATES 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 BUTENEITRILES OF THE FORMULA: NC-C(-HALO)=C (-CF3)-NH-C(=X)-NH-R PYRIMIDINE WHEREIN R IS ALKYL, ALKENYL, PHENYL, BENZYL AND SUBSITUTED DERIVATIVES THEREOF AND X IS SULFUR OR OXYGEN. THE UREIDO BUTENENITRILES ARE TREATED WITH ADDITIONAL BASE TO PRODUCE NOVEL CYCLIC CYTOSINES OF THE FORMULA; 2(=X),3-R,4-(=NH),5-(HALO-),6-(F3C-)-1,2,3,4-TETRAHYDRO WHEREIN R AND X ARE AS DEFINED ABOVE. THE CYTOSINES CAN BE PRODUCED DIRECTLY BY TREATING 3-AMINO-2-SUBSITUTED4,4,4-TRIFLUORO-2-BUTENENTRILE WITH AT LEAST 1.0 MOLE EQUIVLAENTS OF BASE. THE NOVEL COMPOUNDS ARE USEFUL INTERMEDIATES IN THE PREPARATION OF HERBICIDAL URACILS AND THIOURACILS.
专利号:US-2003068317-A1 优先权日:2001-04-20 标题:High capacity methods for separation, purification, concentration, immobilization and synthesis of compounds and applications based thereupon 发明人:LEE WILLIAM; SAITO KYOICHI 摘要:Compositions are provided herein comprising a base material having engrafted polymer brushes. The polymer brushes further comprise one or more functional groups immobilized along the surface of the brushes in a plurality of layers, which confer functional properties to the base material compositions. Methods of using these compositions include deoxygenation of a sample solution, hydrolysis of denaturing agents in a sample solution, resolution of racemic mixtures in a sample solution, and purification, and concentration of target compounds.
专利号:US-2008070274-A1 优先权日:2001-12-10 标 题 :High capacity, methods for separation, purification, concentration, immobilization and synthesis of compounds and applications based thereupon 发明人:LEE WILLIAM; SAITO KYOICHI 权利人:LEE WILLIAM; SAITO KYOICHI 摘要:Compositions are provided herein comprising a base material having engrafted polymer brushes. The polymer brushes further comprise one or more functional groups immobilized along the surface of the brushes in a plurality of layers, which confer functional properties to the base material compositions. Methods of using these compositions include deoxygenation of a sample solution, hydrolysis of denaturing agents in a sample solution, resolution of racemic mixtures in a sample solution, and purification, and concentration of target compounds.