专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:WO-2008101515-A1 优先权日:2007-02-22 标 题:New synthons for the synthesis of chiral peptide nucleic acids and methods for preparing the same 发明人:BIONDI FABIO 权利人:NANODREAM S R L UNIPERSONALE; BIONDI FABIO 摘要:Novel l-acyl-3-amino-4-hydroxymethylpyiÏ„olidine derivatives useful as PNA synthons optionally having protecting groups suitable of removal under mild conditions are disclosed having the formula (E) wherein: R1 is H or R-C(=O), wherein R is straight or branched alkyl, aryl, substituted aryl including from 1 to 5 heteroatoms, a heterocyclic group including from 1 to 3 heteroatoms; R2 is H, a linker bonded to a solid support, or R6-0-C(=0), wherein R6 is an alkyl or substituted alkyl group having a tertiary carbon atom bonded to the oxygen, CHn-Arm-n wherein n is 1 or 2 and m is 2 or 3 and Ar is aryl or substituted aryl, and R3 is a nucleobase selected from thymine I, cytosine II, adenine III, guanine IV, uracil V, xanthine VI and hypoxanthine VII, a derivative of said nucleobases I-VII protected at the reactive functionalities NH2 or imidic NH, a deazacarbocyclic derivative of said nucleobases I-VII optionally protected at the reactive functionality NH2. Also disclosed are novel intermediates useful for the preparation of the aforementioned PNA synthons, as well as to methods for preparing the intermediates and the final synthons. The latter can be useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers.
专利号:US-2022356139-A1 优先权日:2019-09-03 标 题:Synthesis of deuterated aldehydes 发明人:WANG WEI 权利人:ARIZONA BOARD OF REGENTS ON BEHALF OF ATHE UNIV OF ARIZONA 摘要:Described are methods for preparing a deuterated aldehyde using N-heterocyclic carbene catalysts in a solvent comprising D 2 O. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions without functionality manipulation.
专利号:US-2018208775-A1 优先权日:2014-06-23 标 题:New aromatic macrocyclic metal complex dyes and the synthesis thereof with active nano metal powders 发明人:OLGUN UGURSOY; YILDIZ SALIH ZEKI 权利人:OLGUN UGURSOY; YILDIZ SALIH ZEKI 摘要:The present invention relates to a new type of inorganic coordination compound dyes having advanced technology optical, electronic and medical characteristics and relates to production of these dyes by means of new synthesis methods. The present invention relates to dyes which are metal (M: Li, Na, K, Mg, Ca, Sr, Ba, Ti, Zr, V, Cr, Mo, Mn, Re, Fe, Ru, Co, Rh, Ir, Ni, Pd, Pt, Cu, Ag, Au, Zn, Cd, B, Al, Ga, In, Si, Ge, Sn, Pb, Sb, Bi, Se, Te) complexes of aromatic macrocyclic compounds of the type Phtalocyanine (Pc), Naphtalocyanine (Nc), Porphyrazine (Pz), Porphyrin (Pr), sub-Phtalocyanine (subPc), sub-Naphtalocyanine (subNc), sub-Porphyrazine (subPz), sub-Porphyrine (subPr), and relates to the synthesis of these complexes and derivatives. The subject matter dyes can be used in solar cell photovoltaic (PV) panels, in OLEDS which are organic structured light emitting diodes, in polymers, in textile and in photodynamic therapy PDT applications. Moreover, industrial applications are possible which depend on strong fluorescence characteristics.
专利号:US-7125983-B2 优先权日:2000-11-29 标题:L-nucleic acid derivatives and process for the synthesis thereof 发明人:IIZUKA HAJIME; TOGASHI KAZUHIKO; SUZUKI TSUNEJI 权利人:MITSUI CHEMICALS INC 摘要:A novel method has been found to produce 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine. A novel method has been further found to L-2′-deoxyribose derivatives as a useful synthetic intermediate through L-2,2′-anhydro-5,6-dihydrocyclouridine derivative. According to these methods, synthesis of various L-nucleic acid derivatives, synthesis of which has been difficult till now.
参考标题:Synthesis OfO-(Dimethylamino)Aryl Ketones And Acridones By The Reaction Of 1,1-Dialkylhydrazones And Arynes 作者:Anton V. Dubrovskiy,Richard C. Larock |发布日期:2011.8.5 摘要:A Novel, Efficient Route To Biologically And Pharmaceutically Important O-(Dimethylamino)Aryl Ketones And Acridones Has Been Developed Starting From Readily Available 1,1-Dimethylhydrazones Of Aldehydes And O-(Trimethylsilyl)Aryl Triflates. The Reaction Proceeds Under Mild Conditions, Tolerates A Wide Range Of Functional Groups, And Provides The Final Products In Good To Excellent Yields.
合成参考文献
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