专利号:US-5712367-A 优先权日:1989-10-02 标 题:Process for the solubilization of peptides and process for peptide synthesis 发明人:BERNARD JEAN-MARIE; BOUZID KAMEL; GERVAIS CHRISTIAN 权利人:RHONE POULENC CHIMIE 摘要:A process is disclosed for making peptides soluble in a water-immiscible organic solvent, comprising linking a lipophilic group with an amide or ester bond to the terminal carboxyl group of said peptide; when the lipophilic group is linked to L-serine, a molecule is obtained with a solubility in water at 25 DEG C. of less than 30 g/liter. This lipophilic group is non-polymeric and chemically defined. A process is also disclosed for the synthesis of peptides, optionally protected, in a liquid medium, wherein the starting material is an amino acid or peptide made soluble in an organic medium by a lipophilic group A-L linked to the carboxyl function of the starting amino acid or peptide, and are added to amino acids or peptides to be condensed which are activated on their acid function and protected on their amine function and are optionally protected on their side chain. The peptides resulting from the synthesis are used, where appropriate, for the synthesis of medicinal products, vaccines or agri-foodstuff or plant-protection.
专利号:US-8710261-B2 优先权日:2005-02-22 标 题:5-phenyl-pentanoic acid derivatives as matrix metalloproteinase inhibitors for the treatment of asthma and other diseases 发明人:PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G 权利人:PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G; RANBAXY LAB LTD 摘要:The present invention relates to Compounds having the structure of Formula I: wherein n is an integer from 1 to 5; R 1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; R 2 is alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R χ , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , C(â•?Y)NR 4 R 5 , C(â•?O)OR 6 [wherein Y is oxygen or sulphur], OR 5 , —O(Câ•?O)NR 4 R 5 , O-acyl, S(O) m R 4 , —SO 2 N(R 4 ) 2 , cyano, amidino or guanidino [wherein R 4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; R 5 is hydrogen or R 4 ; R x is R 4 or —SO 2 N(R 4 ) 2 and R 6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; R 3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR 4 , —OC(â•?O)NR 4 R 5 , O-acyl, NH 2 , NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R x , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , and to processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterize by over-expression and over-activation of an matrix metalloproteinase, using the compounds.
专利号:US-9272260-B2 优先权日:2009-08-14 标 题 :Methods of synthesis and purification by use of a solid support 发明人:HAMMOND GERALD B; XU BO 权利人:HAMMOND GERALD B; XU BO; UNIV LOUISVILLE RES FOUND 摘要:Disclosed herein are novel methods of using polymeric adsorbent resin for chemical synthesis and the purification of product therefrom. Also disclosed herein is a novel method of using silica gel for the combination of chemical reaction and chromatography into a single step. The methods disclosed herein increase the efficiency of chemical synthesis processes. Accordingly, the utility of the methods disclosed herein includes the ability to automate chemical synthesis and purification of the resulting products.
专利号:US-6147159-A 优先权日:1998-09-30 标 题 :Compositions for organic synthesis on solid phase and methods of using the same 发明人:HU YONGHAN; LABADIE JEFFREY W; PORCO JR JOHN ANTHONY; TROST BARRY MARTIN 权利人:ARGONAUT TECHNOLOGIES 摘要:A modified solid support for use in solid phase synthesis which comprises: a solid support having a linker group extending therefrom having the general formula: wherein R1 and R2 are each independently selected from the group consisting of alkyl, cycloalkyl, aryl, alkoxy, aryloxy, fluorine, chlorine, iodine and bromine.
专利号:US-9006491-B2 优先权日:2009-10-22 标题 :Structure and method for synthesizing and using dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine and its tetrafluoroborate 发明人:MA SHENGMING; LÜ BO; FU CHUNLING 权利人:MA SHENGMING; LÜ BO; FU CHUNLING; UNIV ZHEJIANG 摘要:The current invention relates to the structure, synthesis of dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate, as well as its applications in the palladium catalyzed carbon-chlorine bond activation for Suzuki coupling reactions and carbon-nitrogen bond formation reactions. The dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate could coordinate with the palladium catalyst to activate the inert carbon-chlorine bond highly selectively and catalyze Suzuki coupling reaction with arylboronic acid or carbon-nitrogen bond formation reaction with organic amines. The current invention uses only one step to synthesize dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine and its tetrafluoroborate is stable in the air. Compared with known synthetic routes of ligands used in activating carbon-chlorine bonds, the method of current invention is short, easy to operate. Moreover, with this type of ligands, the Suzuki coupling products of optically active chlorolactones and arylboronic acids would maintain their configuration and optical purity.
专利号:CN-117865845-A 优先权日:2024-01-22 标题 :Application of ferric oxide to catalytic three-step series atom economic synthesis of imine or derivative thereof by using aromatic nitro compound and benzyl alcohol compound
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合成参考文献
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