CAS: 4530-20-5; Boc-Gly-Oh

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Perylen-3-Ylmethyl 2-((Tert-Butoxycarbonyl)Amino)Acetate置于水体系中,用 乙腈 作为反应溶剂,以95%的收率获得产物boc-甘氨酸
参考文献:Perylen-3-Ylmethyl:用于羧酸和醇的荧光光可去除保护基(fprpg)
标题:Perylen-3-Ylmethyl:用于羧酸和醇的荧光光可去除保护基(fprpg)
摘要:Perylen-3-Ylmethyl被证明是一种用于羧酸和醇的新型荧光光可去除保护基(fprpg).包括氨基酸在内的羧酸通过与fprpg脯氨酸-3-基甲基偶联而作为相应的酯得到保护.笼状酯的光物理研究表明它们都具有很强的荧光特性,其荧光量子产率在0.85-0.95范围内.使用可见光(>=410Nm)在乙腈水溶液中对笼形酯进行辐照,可以释放出相应的羧酸,其化学成分较高(94-97%),量子产率为(0.072-0.093).笼型酯在不同溶剂中的光解结果表明,溶剂对光释放速率有影响.此外,我们还探索了fprpg的功能,
DOI:10.1016/j.Tet.2011.11.074

专利信息

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:US-5760237-A
优先权日:1995-08-25
标 题 :Synthesis of l-azatyrosine using pseudoephedrine as a chiral auxiliary
发明人：MYERS ANDREW G
权利人:CALIFORNIA INST OF TECHN
摘要:A practical synthesis of the potential chemotherapeutic agent L-azatyrosine is described. The key step involved the alkylation of (R,R)-(-)-pseudoephedrine glycinamide with 5-benzenesulfonyloxy-2-iodomethylpyridine and proceeded in 70-95% yield and 89-95% de. Simultaneous hydrolysis of the auxiliary and the benzenesulfonate protecting group afforded L-azatyrosine of ≧99% ee in 73% yield on multigram scale (recovery yield of (R,R)-(-)-pseudoephedrine: 90%).

专利号:US-7589170-B1
优先权日:1998-09-25
标题 :Synthesis of cyclic peptides
发明人：SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER
权利人:UNIV QUEENSLAND
摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.

专利号:US-5026773-A
优先权日:1987-03-11
标 题 :Apparatus for a solid phase synthesis of peptide analogs
发明人：STEEL SAMUEL
权利人:STEEL SAMUEL
摘要:A novel polymeric disc, wafer or similarly shaped resin for carrying out the synthesis of peptide analogs via solid phase peptide synthesis techniques is provided. The polymeric disc or wafer of the invention may be made out of those resin materials presently used in bead form in solid phase peptide synthesis, such as, benzhydrylamine resins, Boc-aminoacyl-4-(oxymethyl)-phenyacetamidomethyl (Pam) resin, polyamide resins and chloromethyl resins. The disc or wafer of the invention should, preferably, have a thickness of 200-400 mu m and may be of any suitable length or width. A process for the synthesis of peptide analogs utilizing the polymeric disc or wafer of the present invention is also disclosed.

专利号:US-2006264608-A1
优先权日:2001-08-03
标题 :Bi-directional synthesis of oligoguanidine transport agents
发明人：WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C
权利人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C
摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.

专利号:EP-2260936-B1
优先权日:2004-11-25
标题:Method for specifically located synthesis of nucleic acids on solid carriers
发明人：ELLINGER THOMAS; ERMANTRAUT EUGEN; HOLZHEY NANCY; PLENZ FRANK; SCHULZ TORSTEN; TUCHSCHEERER JENS; WEICHERDING DANIEL
权利人:CLONDIAG GMBH
摘要:Type-specific synthesis of bio-polymers of a defined sequence on pre-determined ranges of a solid carrier comprises gradual coupling of monomer and/or oligomer components (I); where, before the coupling step, at least a pre-determined area of the carrier are activated for coupling of (I) to activate the reactive groups; and the temporary group for protection are removed by addition of an activation reagent in aqueous solution, is new. Independent claims are also included for: (1) a procedure for the type-specific synthesis of biopolymers of a defined sequence on pre-determined ranges of solid carrier, comprising: (a) arranging a mask on the carrier (for coupling of (I) of the biopolymer, which is to be synthesized for controlling available reactive groups with protection groups to the carrier); (b) activating the reactive groups by removing the temporary protective groups at the ranges given by the mask, by adding the activation reagent in aqueous solution; (c) coupling (I) with activated reactive groups; and (d) repeating step (a) to (c), until the desired biopolymers is synthesized; (2) a micro array prepared by the process; and (3) a micro array with pre-determined ranges immobilized biopolymer probes, where the proportional portion P at biopolymers, which exhibits the desired number of monomer M, is given by the formula P = S-M (where S is an average step yield with the coupling of (I); and the density at pre-determined ranges is at least 1500 spots per cm 2>and the average step yield is 95 (preferably 98) %).