2-甲基-4,5-二氢-1,3-噻唑-4-羧酸甲酯置于盐酸,水体系中,化学反应 24.0H,以94%的收率获得产物l-半胱氨酸盐酸盐无水物 参考文献:Efficient Synthesis Of Primary 2-Aminothiols From 2-Aminoalcohols And Methyldithioacetate 标题:Efficient Synthesis Of Primary 2-Aminothiols From 2-Aminoalcohols And Methyldithioacetate 摘要:Various Primary 2-Aminothiols Have Been Prepared By A General And Efficient Method,In Three Steps,Starting From Commercially Available 2-Aminoalcohols And Methyldithioacetate As A Convenient Source Of Sulfur. (C) 2008 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Tetlet.2008.09.014
专利号:US-5824472-A 优先权日:1986-03-24 标 题 :Process for the synthesis of sugar nucleotides using recombinant-DNA methods 发明人:BETLACH MICHAEL R; DOHERTY DANIEL H; VANDERSLICE REBECCA W 权利人:MONSANTO CO 摘要:A recombinant-DNA mediated method for the synthesis of sugar nucleotides is disclosed. This method utilizes portable DNA sequences capable of directing the microbial synthesis of various enzymes that catalyze the synthesis of sugar nucleotides, including UDP-glucose, UDP-glucuronic acid and GDP-mannose. The sugar moieties of these sugar nucleotides may subsequently be incorporated into industrially-useful polysaccharides such as xanthan gum. It has been found that vectors containing the portable DNA sequences described herein are capable both of causing sugar nucleotide production in microorganisms previously incapable of such synthesis and of causing increased sugar nucleotide production in organisms capable of synthesizing small quantities of these compounds. In particular, plasmids pAS7, pAS9 and pTS13 are disclosed. These plasmids are capable of directing sugar nucleotide synthesis in various hosts, including Xanthomonas sp. such as X. campestris and other organisms such as E. coli and various Pseudomonas sp.
专利号:US-7230101-B1 优先权日:2002-08-28 标 题:Synthesis of methotrexate-containing heterodimeric molecules 发明人:MURTHI KRISHNA K; SMITH CHASE C 权利人:GPC BIOTECH INC 摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:
专利号:US-6579725-B1 优先权日:1999-03-05 标题 :Linkers for synthesis of oligosaccharides on solid supports 发明人:SEEBERGER PETER H; ANDRADE RODRIGO B 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention relates to versatile linkers for tethering a molecule to a solid support, e.g., for tethering a monomer, oligomer or polymer to a solid support, which are stable to a wide range of reaction conditions, but can be cleaved under well-defined conditions, thereby liberating the molecule from the solid support. Preferably, the linkers are used to tether to the solid support unprotected, partially-protected or fully-protected monosaccharides or oligosaccharides, or unprotected, partially-protected or fully-protected glycoconjugates. The linkers of the present invention may be used to tether to solid supports building blocks useful in the assembly of libraries of other types of small molecules. The present invention also relates to a molecule or plurality of molecules tethered to the solid support via a linker or linkers of the present invention. The present invention also relates to processes for synthesizing molecules, e.g., monomers, oligomers or polymers, on a solid support, wherein a starting material in the synthesis of the molecule, intermediates in the synthesis of the molecule, and the molecule itself are tethered to the solid support during the process via one of the linkers of the present invention. In certain processes of the present invention, the molecule is liberated from the solid support by cleavage of the linker of the present invention.
专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:US-12018313-B2 优先权日:2016-12-28 标题:Methods, apparatuses, and systems for microorganism strain analysis of complex heterogeneous communities with tracer analytics, determination of functional relationships and interactions thereof, and synthesis of microbial ensembles 发明人:EMBREE MALLORY 权利人:NATIVE MICROBIALS INC 摘要:Methods, apparatuses, and systems for microorganism strain analysis of complex heterogeneous communities with tracer analytics, determination of functional relationships and interactions thereof, and synthesis of microbial ensembles, including dosed microbial ensembles and inoculative microbial ensembles, are disclosed.
专利号:US-6846917-B2 优先权日:2001-01-23 标题:Solid- and solution-phase synthesis of heparin and other glycosaminoglycans 发明人:SEEBERGER PETER H; ORGUEIRA HERNAN; SCHELL PETER 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Described is a modular, general synthetic strategy for the preparation in solution and on a solid support of heparin, heparin-like glycosaminoglycans, glycosaminoglycans and non-natural analogs of each of them. Additionally, the modular strategy provides the basis for the preparation of combinatorial libraries and parallel libraries of defined glycosaminoglycan oligosaccharides. The defined glycosaminoglycan structures may be used in high-throughput screening experiments to identify carbohydrate sequences that regulate a host of recognition and signal-transduction processes. The determination of specific sequences involved in receptor binding holds great promise for the development of molecular tools which will allow modulation of processes underlying viral entry, angiogenesis, kidney diseases and diseases of the central nervous system. Notably, the present invention enables the automated synthesis of glycosaminoglycans in much the same fashion that peptides and oligonucleotides are currently assembled.
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合成参考文献
参考文献:10.1038/nbt.2488 摘要:Thiele I, Swainston N, Fleming RMT, Hoppe A, Sahoo S, Aurich MK, Haraldsdottir H, Mo ML, Rolfsson O, Stobbe MD, Thorleifsson SG, Agren R, Bölling C, Bordel S, Chavali AK, Dobson P, Dunn WB, Endler L, Hala D, Hucka M, Hull D, Jameson D, Jamshidi N, Jonsson JJ, Juty N, Keating S, Nookaew I, Le Novère N, Malys N, Mazein A, Papin JA, Price ND, Selkov E, Sigurdsson MI, Simeonidis E, Sonnenschein N, Smallbone K, Sorokin A, van Beek JHGM, Weichart D, Goryanin I, Nielsen J, Westerhoff HV, Kell DB, Mendes P, Palsson BØ. A community-driven global reconstruction of human metabolism. Nature Biotechnology. 2013 Mar 03;31(5):419–25. doi: 10.1038/nbt.2488.