专利号:US-7893286-B2 优先权日:2007-06-01 标题 :Method for the synthesis of phospholipid ethers 发明人:PINCHUK ANATOLY; WEICHERT JAMEY P; LONGINO MARC 权利人:CELLECTAR INC 摘要:Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.
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-9550801-B2 优先权日:2009-04-06 标 题:Synthesis of four coordinated platinum complexes and their applications in light emitting devices thereof 发明人:LI JIAN; WANG ZIXING; TURNER ERIC 权利人:ARIZONA BOARD OF REGENTS ACTING FOR AND ON BEHALF OF ARIZONA STATE UNIV 摘要:Platinum complexes that exhibit photoabsorption and photoemission, methods of making such complexes, and applications thereof are disclosed, including optical devices comprising the complexes.
专利号:US-5591867-A 优先权日:1992-12-04 标 题 :Synthesis of kainic acid 发明人:MONN JAMES A 权利人:LILLY CO ELI 摘要:This invention provides a process for preparing kainic acid and provides intermediates in the synthesis thereof.
专利号:WO-2008101514-A1 优先权日:2007-02-22 标 题:Nucleoside analogues for the treatment of viral infections and methods for preparing them 发明人:BIONDI FABIO 权利人:NANODREAM S R L UNIPERSONALE; BIONDI FABIO 摘要:New pyrrolidine derivatives are disclosed having formula (I) wherein R1 and R2 are protecting groups independently selected from R-C(=O), wherein R is straight or branched C1-C15 alkyl, C6-C15 aryl, substituted C5-C15 aryl including from (1) to (5) heteroatoms and R3 is a nucleobase selected from thymine I, cytosine II, adenine III, guanine IV, uracile 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. These pyrrolidine derivatives are nucleoside isosteres and can be employed for the synthesis of DNA chimeras or as termination sequences for diagnostic and therapeutic applications. Also disclosed are novel intermediates useful for the preparation of the aforementioned pyrrolidine derivatives, as well as to methods for preparing both the intermediates and the final pyrrolidine derivatives.
专利号:US-10759743-B2 优先权日:2016-10-24 标 题 :Pd-catalyzed γ-C(sp3)-H arylation / heteroarylation of free amines 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.