📜(R)-(-)-2-氨基庚烷置于2,2,2-三氟乙硫醇体系中,用 四氢呋喃,3-甲基-3-戊醇 用作溶剂,化学反应 2.0H,反应生成异庚胺 参考文献:En Route To (S)-Selective Chemoenzymatic Dynamic Kinetic Resolution Of Aliphatic Amines. One-Pot Kr/racemization/kr Sequence Leading To (S)-Amides 标题:En Route To (S)-Selective Chemoenzymatic Dynamic Kinetic Resolution Of Aliphatic Amines. One-Pot Kr/racemization/kr Sequence Leading To (S)-Amides 摘要:A One-Pot Sequential Process,Involving A Radical Racemization And An Enzymatic Resolution,Provides Access To (S)-Amides,From Racemic Amines,With Ee And Yields Ranging From 78 To 94% And 58 To 80%,Respectively. Doi:10.1021/jo900074W
专利号:US-2005130201-A1 优先权日:2003-10-14 标 题 :Splint-assisted enzymatic synthesis of polyribounucleotides 发明人:DERAS MICHAEL; PLEISS JEFFREY A; SCARINGE STEPHEN 权利人:DHARMACON INC 摘要:The present invention comprises methods and compositions for splint-assisted enzymatic synthesis of polyribonucleotides using an RNA polymerizing enzyme. The invention provides ligating ribonucleotides comprising ligating a donor RNA molecule to an acceptor RNA molecule in the presence of RNA ligase and a splint, wherein the donor RNA molecule is comprised of at least one nucleotide and a ligation linker moiety, the acceptor RNA molecule is comprised of at least one nucleotide and a ligation linker moiety and the splint is comprised of a polyribonucleotide. The invention also provides splints for use in splint-assisted enzymatic synthesis using an RNA polymerizing enzyme.
专利号:US-2008206850-A1 优先权日:2007-02-28 标 题:Methods and compositions for DNA synthesis 发明人:DELLINGER DOUGLAS J; DELLINGER GERALDINE F; CARUTHERS MARVIN H 权利人:DELLINGER DOUGLAS J; DELLINGER GERALDINE F; CARUTHERS MARVIN H 摘要:In some embodiments, the present disclosure relates to new phosphoramidite compositions, that have Silyl-containing carbonate or thiocarbonate or ether as 5′-hydroxyl protecting groups useful of the synthesis of DNA, and in particular for the synthesis of long sequences of DNA (e.g., >50 mer). In some embodiments, there are provided methods for simultaneous oxidation of the internucleoside phosphate triester linkages and removal of the 5′-hydroxyl-protecting group, making this process a new 2-step DNA synthesis, that involves the use of peroxyanions in combination with fluoride anions.
专利号:US-2008206851-A1 优先权日:2007-02-28 标题:Methods and compositions for RNA synthesis 发明人:DELLINGER DOUGLAS J; DELLINGER GERALDINE F; CARUTHERS MARVIN H 权利人:DELLINGER DOUGLAS J; DELLINGER GERALDINE F; CARUTHERS MARVIN H 摘要:In some embodiments, the present disclosure relates to new phosphoramidite compositions, that have Silyl-containing carbonate or thiocarbonate or ether as 5′-hydroxyl protecting groups useful fo the syntheis of RNA, and in particular for the synthesis of long sequences of RNA (e.g., >50 mer). In some embodiments, there are provided methods for simultaneous oxidation of the internucleoside phosphate triester linkages and removal of the 5′-hydroxyl-protecting group, making this process a new 2-step RNA synthesis, that involves the use of peroxyanions in combination with fluoride anions.
专利号:US-7193077-B2 优先权日:2003-08-30 标 题 :Exocyclic amine triaryl methyl protecting groups in two-step polynucleotide synthesis 发明人:DELLINGER DOUGLAS J; SIERZCHALA AGNIESZKA B; CARUTHERS MARVIN H 权利人:AGILENT TECHNOLOGIES INC 摘要:Precursors for use in the synthesis of polynucleotides and methods of using the precursors in synthesizing polynucleotides are disclosed. The precursors include a heterocyclic base having an exocyclic amine group and a substituted or unsubstituted triaryl methyl protecting group bound to the exocyclic amine group.
专利号:US-7427679-B2 优先权日:2003-08-30 标 题:Precursors for two-step polynucleotide synthesis 发明人:DELLINGER DOUGLAS J; SIERZCHALA AGNIESZKA B; CARUTHERS MARVIN H 权利人:AGILENT TECHNOLOGIES INC 摘要:Precursors for use in the synthesis of polynucleotides are disclosed. The precursors include a heterocyclic base having an exocyclic amine group and a substituted or unsubstituted triaryl methyl protecting group bound to the exocyclic amine group. In particular embodiments, the precursor has the structure: n nwherein:n O and H represent oxygen and hydrogen, respectively, R 1 is hydrido, hydroxyl, protected hydroxyl, lower alkyl, modified lower alkyl, or alkoxy, one of R 2 or R 3 is a hydroxyl protecting group; and the other of R 2 or R 3 is a reactive group capable of reacting with a reactive site hydroxyl, Base is a heterocyclic base having an exocyclic amine group, and Tram is a triaryl methyl group having the structure (V) n nwherein the broken line represents a bond to the amino nitrogen of the exocyclic amine group, and R 4 , R 5 and R 6 are independently selected from unsubstituted or substituted aryl groups, provided that at least one of R 4 , R 5 , and R 6 is an aryl group other than phenyl and other than substituted phenyl.
专利号:US-8309706-B2 优先权日:1998-08-03 标 题 :Methods of synthesizing oligonucleotides using carbonate protecting groups and alpha-effect nucleophile deprotection 发明人:DELLINGER DOUGLAS J; CARUTHERS MARVIN H; BETLEY JASON R 权利人:DELLINGER DOUGLAS J; CARUTHERS MARVIN H; BETLEY JASON R; AGILENT TECHNOLOGIES INC 摘要:The invention provides methods for synthesizing oligonucleotides using nucleoside monomers having carbonate protected hydroxyl groups that are deprotected with α-effect nucleophiles. The α-effect nucleophile irreversibly cleave the carbonate protecting groups while simultaneously oxidizing the internucleotide phosphite triester linkage to a phosphodiester linkage. The procedure may be carried out in aqueous solution at neutral to mildly basic pH. The method eliminates the need for separate deprotection and oxidation steps, and, since the use of acid to remove protecting groups is unnecessary, acid-induced depurination is avoided. Fluorescent or other readily detectable carbonate protecting groups can be used, enabling monitoring of individual reaction steps during oligonucleotide synthesis. The invention is particularly useful in the highly parallel, microscale synthesis of oligonucleotides.
1: Almeida CVP, Neng NR, Nogueira JMF, Ruivo J. Application of a bar adsorptive microextraction based methodology for doping control of alkylamine stimulants in urine matrices. J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Feb 15;1234:124006. doi: 10.1016/j.jchromb.2024.124006. Epub 2024 Jan 10. 88(3):38-43. Russian. doi: 10.17116/otorino20228803138. 87(4):79-83. Russian. doi: 10.17116/otorino20228704179. 173:447-453. doi: 10.1016/j.colsurfb.2018.10.015. Epub 2018 Oct 9. 46(4):1211-4. doi: 10.1183/13993003.00051-2015. Epub 2015 Jul 23. 114:668-80. doi: 10.1016/j.saa.2013.05.097. Epub 2013 Jun 4. 108(38):15810-5. doi: 10.1073/pnas.1106030108. Epub 2011 Sep 1.
合成参考文献
摘要:Rodríguez-Mata, M.; Gotor-Fernández, V., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 208. 摘要:Adriaensen, K.; De Vos, D., Science of Synthesis, (2022) , 163. 摘要:Adriaensen, K.; De Vos, D., Science of Synthesis, (2022) , 167. 摘要:Journal of the American Pharmaceutical Association, Scientific Edition., 30(623), 1941 摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664