专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:WO-2012017400-A1 优先权日:2010-08-03 标 题 :Synthesis of acyl-pantetheine derivatives and the use thereof in the synthesis of acyl-coenzyme a derivatives 发明人:VAN DIJK ALBERDINA AIKE; BADENHORST CHRISTOFFEL PETRUS STEPHANUS 权利人:UNIV NORTHWEST; VAN DIJK ALBERDINA AIKE; BADENHORST CHRISTOFFEL PETRUS STEPHANUS 摘要:The present invention relates to a novel synthesis method for acyl-pantetheine derivatives. The present invention further relates to the use of said synthesized acyl-pantetheine derivatives as a starting material in the enzymatic synthesis of acyl-coenzyme A derivatives. According to a first aspect thereof, the present invention provides a method for the synthesis of acyl-pantetheine derivatives, the method including the steps of: a) providing a source of pantetheine; b) providing a source of acyl ester; and c) contacting the source of pantetheine with the source of acyl ester to form the corresponding acyl-pantetheine derivative, having the general formula (I), wherein R is an acyl group.The present invention also provides a method for the synthesis of acyl-coenzyme A derivatives as well as the use of a source of pantetheine and a source of acyl ester in the preparation steps of these two methods.
专利号:US-8138330-B2 优先权日:2006-09-11 标 题 :Process for the synthesis of oligonucleotides 发明人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED 权利人:LEUCK MICHAEL; WOLTER ANDREAS; STUMPE ALFRED; SIGMA ALDRICH CO LLC 摘要:The present invention discloses novel methods for the synthesis of oligonucleotides with nucleoside phosphoramidites on solid supports. The methods comprise the stepwise chain assembly of oligonucleotides on supports with 5′-acyl phosphoramidites. The synthesis cycles consist of a front end deprotection step which is conducted with a solution of a primary amine or a phenolate, a phosphoramidite coupling step with a 5′-acyl nucleoside phosphoramidite in the presence of an activator, a phosphite oxidation step and an optional capping step. The novel methods improve the quality of synthetic oligonucleotides due to the irreversibility of the front end deprotection step, which prevents the formation of deletion sequences, and due to the avoidance of acidic reagents in the synthesis cycles, which prevent the formation of depurination side products. The invention further discloses novel nucleoside phosphoramidite compositions wherein the phosphoramidites carry acyl front end protective groups which are cleavable with primary amines or phenolates. The invention is applicable to the synthesis of oligodeoxyribonucleotides, oligoribonucleotides and oligonucleotides with modifications in their sugar or phosphate groups.
专利号:WO-9817677-A1 优先权日:1996-10-24 标 题 :Improvements in solid-phase synthesis of peptides and related compounds 发明人:ENGLEBRETSEN DARREN 权利人:UNIV QUEENSLAND; ENGLEBRETSEN DARREN 摘要:The invention relates to spacers for use in solid-phase synthesis of peptides and peptide-related compounds, in which a spacer construct is used to ensure that the target peptide or peptide-related compound is at a distance equivalent to at least 5-15 amino acids from the solid support. Constructs of the invention are particularly applicable to the synthesis of strongly hydrophobic peptide, which are otherwise difficult, if not impossible to purify and analyse. The constructs and methods of the invention are also applicable to synthesis of peptide nucleic acids.
专利号:US-5648537-A 优先权日:1995-01-24 标题 :Process for the synthesis of substituted carbodiimides 发明人:HUSSENET PATRICIA; LE GOFF PHILIPPE; SENNYEY GERARD 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The invention relates to a new process for the synthesis of a disubstituted carbodiimide, including a first stage of phosgenation of an N,N'-disubstituted urea in an organic solvent medium. n After this first stage ammonia is added to the reaction mixture without preliminary isolation of any intermediate compound. n The process is simple, relatively inexpensive and the yield is high. n Disubstituted carbodiimides are organic synthesis intermediates used especially in pharmaceutical chemistry as coupling agents in peptide synthesis.
专利号:WO-0100609-A1 优先权日:1999-06-29 标题:Method for synthesis of n-homocysteine thiolactonyl retinamide 发明人:KAZIMIR MICHAEL; WILSON RAY E II 权利人:UNIV BAYLOR; KAZIMIR MICHAEL; WILSON RAY E II 摘要:The present invention describes methods of synthesis for N-homocysteine thiolactonyl retinamide (thioretinamide), a compound that has anticancer and antiatherogenic properties. The present invention further describes methods for the synthesis of N-homocysteine thiolactonyl retinamido cobalamin (thioretinaco), a compound that has potential anticancer, antineoplastic, antiviral, and antiatherogenic properties.
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合成参考文献
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