专利号:US-12012427-B2 优先权日:2019-10-31 标 题 :Synthesis of Fmoc-protected morpholino monomers and their use in the synthesis of morpholino oligomer 发明人:SINHA SURAJIT; KUNDU JAYANTA; GHOSH UJJWAL 权利人:INDIAN ASS FOR THE CULTIVATION OF SCIENCE 摘要:Present invention relates to stable Fmoc protected Morpholino monomers and corresponding oligonucleotides (PMO) and efficient synthesis of the same involving chlorophosphoramidate and H-Phosphonate chemistry. Successful syntheses of the oligonucleotide with higher yield and lesser time have been accomplished employing solid phase synthesis and easy deprotection of Fmoc group with Piperidine.
专利号:US-11891375-B2 优先权日:2021-07-26 标 题 :Method for the synthesis of 2,4-dimethylpyrimidin-5-ol, intermediates, and method for the synthesis of Lemborexant using the intermediates 发明人:AKHATOU ABDESLAM; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.
专利号:US-10450201-B2 优先权日:2017-10-04 标题 :Method for the synthesis of nanoparticles of heterometallic nanocomposite materials 发明人:SOHAIL MANZAR; SHARIF MUHAMMAD; KHAN SAFYAN A; SHER MUHAMMAD; JAGADEESH RAJENAHALLY V 权利人:UNIV KING FAHD PET & MINERALS 摘要:A simple one pot sol-gel method for the synthesis of bi-metal nanostructures is based on non-noble metals (Fe, Co and Sn) and titanium. The method involves the synthesis of mixed metal nanoscale composites using low cost precursors which allow for the synthesis of desired nanocomposite materials with self-scarifying titanium or silica supports. The procedure does not require any surfactant or any need for pH controlled step. Applicants' method involves the in-situ generation of precursors and their simultaneous entrapment in a gel. This simple one pot synthesis allows for the synthesis of homogenous size, shape and distribution of targeted nanostructures. Further, this method can be applied for the preparation of various nanocomposite materials using different choices of metals and self-scarifying supports. Applicants also show that Pd, the noble metal based nanocomposite is feasible.
专利号:US-7329515-B2 优先权日:2003-04-21 标题 :Solid support for the synthesis of 3′-amino oligonucleotides 发明人:LEUCK MICHAEL; WOLTER ANDREAS 权利人:SIGMA ALDRICH CO 摘要:The present invention discloses novel methods and solid supports for the synthesis of 3′-amino oligonucleotides. The novel supports are based on an unsubstituted or ring-substituted hydroxymethylbenzoyl linker element wherein the hydroxymethyl group is esterified to a solid phase bound carboxylic acid and the carbonyl group is linked to an amino alcohol as an amide. Oligonucleotides are conveniently synthesized on the novel supports with no modifications in the standard phosphoramidite synthesis scheme. The ester function of the support is cleaved under the alkaline deprotection conditions for oligonucleotides to provide a free hydroxymethyl group that aids in the release of the 3′-amino oligonucleotide products with a free amino group through neighbor group participation. The free amino group of the oligonucleotides is available for further conjugation reactions to haptens, reporter groups, surfaces or other small molecules or biomolecules. The methods provided are particularly mild, do not require any modifications in standard protocols for the synthesis and deprotection of oligonucleotides, provide the 3′-amino oligonucleotides free of side products and do not introduce chiral centers to the oligonucleotides.
专利号:US-7956011-B2 优先权日:2005-05-04 标题:Materials and methods for the photodirected synthesis of oligonucleotide arrays 发明人:SERAFINOWSKI PAWEL JERZY; GARLAND PETER BRYAN 权利人:CANCER RES INST ROYAL 摘要:Materials and methods for photodirected synthesis of oligonucleotide arrays on a solid substrate by photodirected synthesis are disclosed which employ a film formed from (i) a photoacid generator that on photolysis generates acid that is capable of directly removing the protecting group of the linker molecules or oligonucleotides and (ii) a polymer substantially lacking electronegative heteroatoms that are capable of hydrogen bonding with photogenerated acid. Methods of synthesizing an oligomer arrays are also described that use a film that restricts diffusion of reactants and products on the substrate during synthesis of the array and which includes a precursor of a deprotecting reagent. The method involves removing one or more of the non-required products of the deprotection reaction from the reactive array elements at which they are produced during the reaction, in order to displace the deprotection reaction towards completion.
专利号:US-9193691-B2 优先权日:2012-04-27 标题:Methods for the synthesis of activated ethylfumarates and their use as intermediates 发明人:KRAFT KELLY SULLIVAN; FREEMAN JOHN J; SERWINSKI PAUL; PAVIA VINNIE; PHANSTIEL OTTO; KAUR NAVNEET 权利人:MANNKIND CORP; MANNKIND CORP 摘要:Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphosphoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.
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