专利号:WO-2013138200-A1 优先权日:2012-03-13 标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof 发明人:FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER 权利人:UNIV HOWARD 摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.
专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-7692016-B2 优先权日:2005-11-25 标 题 :Process for the synthesis of quinoline derivatives 发明人:MADUGULA SREE RAMA MURTY; THALLAPELLY SWAMY; BANDARUPALLY JYOTHIRMAI; YADAV JHILLU SINGH 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides an improved process for the synthesis of quinoline derivatives. More particularly the present invention provides an improved and economical process for the synthesis of quinoline derivatives by the reaction of aniline/substituted anilines using two different catalysts, ferric chloride and zinc chloride in a one-pot set up reaction.
专利号:US-4801744-A 优先权日:1985-03-01 标 题 :Catalytic synthesis of urea from carbon monoxide and amine compound 发明人:HERMAN JEAN-JACQUES; LECLOUX ANDRE 权利人:SOLVAY 摘要:Process for the catalytic synthesis of nitrogen-containing organic compounds, comprising the reaction of carbon monoxide with at least one amino compound in a reaction mixture containing a catalyst based on selenium and a substituted pyridine. The process is particularly suitable for the synthesis of ureas and of their polymers.
专利号:US-2006128930-A1 优先权日:2004-12-03 标题 :Synthesis of sterically hindered phenol based macromolecular antioxidants 发明人:DHAWAN ASHISH; CHOLLI ASHOK L 权利人:DHAWAN ASHISH; CHOLLI ASHOK L 摘要:Disclosed is a method for the synthesis of sterically hindered polymeric antioxidants based on phenol type antioxidant monomers. The method includes polymerizing and alkylating a phenol containing monomer represented by the following structural formula: n n nto produce a sterically hindered polymeric macromolecular antioxidant. X, R 10 and q are as defined herein. The disclosed method is a simple, direct and economical process for the synthesis of sterically hindered polymeric macromolecular antioxidants.
专利号:US-2005130201-A1 优先权日:2003-10-14 标 题 :Splint-assisted enzymatic synthesis of polyribounucleotides 发明人:DERAS MICHAEL; PLEISS JEFFREY A; SCARINGE STEPHEN 权利人:DHARMACON INC 摘要:The present invention comprises methods and compositions for splint-assisted enzymatic synthesis of polyribonucleotides using an RNA polymerizing enzyme. The invention provides ligating ribonucleotides comprising ligating a donor RNA molecule to an acceptor RNA molecule in the presence of RNA ligase and a splint, wherein the donor RNA molecule is comprised of at least one nucleotide and a ligation linker moiety, the acceptor RNA molecule is comprised of at least one nucleotide and a ligation linker moiety and the splint is comprised of a polyribonucleotide. The invention also provides splints for use in splint-assisted enzymatic synthesis using an RNA polymerizing enzyme.
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