专利号:US-5665598-A 优先权日:1994-04-13 标题:Synthesis of chiral N-protected-α-substituted-glycine free acids by zinc-mediated addition of organic halide to glycine cation equivalent 发明人:ABOOD NORMAN A; NOSAL ROGER A 权利人:SEARLE & CO 摘要:A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with alpha -chymotrypsin provides N-Boc-L-propargylglycine in high yield.
专利号:US-11708320-B2 优先权日:2018-06-29 标 题:Environmentally-friendly hydroazidation of olefins 发明人:XU HAO 权利人:UNIV GEORGIA STATE RES FOUND 摘要:The present invention provides processes for the synthesis of organic azides, intermediates for the production thereof, and compositions related thereto.
专利号:US-11679168-B2 优先权日:2018-09-14 标 题 :Caspase-3-triggered molecular self-assembling PET probes and uses thereof 发明人:RAO JIANGHONG; CHENG YUNFENG; CHEN MIN; XIE JIANGHANG; CHEN ZIXIN 权利人:UNIV LELAND STANFORD JUNIOR; THE BOARD OF TRUSTEES OF LELAND STANFORD JUNIOR UNIV 摘要:Embodiments of the synthesis, radiolabeling and biological applications of an activatable tracer that undergoes intramolecular cyclization and aggregation upon activation by cleavage of a blocking moiety are provided. The probes of the disclosure allow for target-controlled self-assembly of small molecules in living subjects for imaging and drug delivery. The aggregated nanoprobes of the disclosure may be detectable optically, by PET detection, magnetic resonance imaging, and the like depending on the detectable reporter attached to the nanoprobe.
专利号:US-10308595-B2 优先权日:2013-02-15 标 题:Albicidin derivatives, their use and synthesis 发明人:SUESSMUTH RODERICH; KRETZ JULIAN; SCHUBERT VIVIEN; PESIC ALEXANDER; HUEGELLAND MANUELA; ROYER MONIQUE; COCIANCICH STEPHANE; ROTT PHILIPPE; KERWAT DENNIS; GRAETZ STEFAN 权利人:UNIV BERLIN TECH 摘要:Antibiotically active compounds characterized by general formula (I), wherein X1, BB, BC, BD, BE and X2 are building blocks with D1, D2, D3, D4 or D5 being linkers which include carbon, sulphur, nitrogen, phosphor and/or oxygen atoms and which are covalently connecting the moities BA and BB, BB and BC, BC and BD, BD and BE and BE and BF, respectively, and wherein in particular the building block BC comprises an amino acid derivative. The compounds for use in a method of treatment of diseases, in particular for use in a method of treatment of bacterial infections are also disclosed.
专利号:US-5508466-A 优先权日:1994-04-13 标题 :Synthesis of N-protected-α-substituted-glycine racemic esters by zinc-mediated addition of organic halide to glycine cation equivalent
专利号:US-8722014-B2 优先权日:2009-05-01 标题 :1 H-[1, 2, 3] triazole substituted amino acids and uses thereof 发明人:MACH ROBERT H; MCCONATHY JONATHAN 权利人:MACH ROBERT H; MCCONATHY JONATHAN; UNIV WASHINGTON 摘要:Tracers for cationic amino acid transport systems and methods of synthesis are disclosed, including compounds comprising a 1H-[1,2,3]triazole moiety. Further disclosed are uses of the analogues, including in vivo imaging of tumors by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).