2,2-二甲基-1,3-二氧戊环-4-甲胺置于硫酸体系中,用 水 作为反应溶剂,化学反应 3.0H,以89%的收率获得产物3-氨基-1,2-丙二醇 参考文献: Process For The Preparation Of A 3-Amino-1,2-Propandiol And Derivatives Thereof[fr] Procédé De Préparation De 3-Amino-1,2-Propandiol Et Ses Dérivés 标题: Process For The Preparation Of A 3-Amino-1,2-Propandiol And Derivatives Thereof[fr] Procédé De Préparation De 3-Amino-1,2-Propandiol Et Ses Dérivés 摘要:制备化合物的过程,其化学式为(i),其中r1和r2分别代表氢或c1至c10烷基基团,通过两步法进行,第一步是在氢气存在下将化合物的化学式为(II)与氨基化合物hnr1 R2进行胺化反应,得到化合物的化学式为(iii),第二步是对化合物的化学式为(iii)进行环裂解反应,得到化合物的化学式为(i).
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-12240835-B2 优先权日:2018-09-18 标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity 发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI 权利人:TERNS PHARMACEUTICALS INC 摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.
专利号:US-8450365-B2 优先权日:2009-05-12 标 题 :Efficient synthesis of galanthamine 发明人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ 权利人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ; UNIV TEXAS 摘要:The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
专利号:US-8383810-B2 优先权日:2004-12-20 标题:Process for the synthesis of azetidinones 发明人:THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 权利人:MERCK SHARP & DOHME; THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 摘要:A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.
专利号:US-2024209018-A1 优先权日:2021-03-22 标题:Universal linker reagents for dna synthesis 发明人:REED MICHAEL W; WU CHENG-HSIEN; COOPER JOHN; DEMPCY ROBERT O 权利人:GENSCRIPT USA INC; CUSTOMARRAY INC 摘要:Provided herein are methods and compositions for oligonucleotide synthesis utilizing universal linker phosphoramidites. Methods and reagents are described with DNA synthesis using controlled pore glass (CPG) solid supports, and on platinum coated electrodes for electrochemical DNA synthesis. The universal linkers can be used as spacers in single-column PCR primer synthesis to generate 2 strands with free 3′-hydroxy termini after cleavage. The methods and compositions utilize a solid support system for synthesis of oligonucleotides, wherein the support has platinum electrodes and a universal linker, optionally wherein the platinum electrode is coated with an amine. The methods and compositions further describe use of universal linker phosphoramidites and the platinum electrode is coated with a monosaccharide, or a disaccharide.
专利号:US-5414077-A 优先权日:1990-02-20 标题 :Non-nucleoside linkers for convenient attachment of labels to oligonucleotides using standard synthetic methods 发明人:LIN KUEI-YING; MATTEUCCI MARK 权利人:GILEAD SCIENCES 摘要:Pseudonucleosides and pseudonucleotides are useful in the synthesis of oligomers which contain these components as a means to derivatize the resulting oligonucleotide to useful substituents such as chelators, intercalators, or lipophilic compounds. In general, these pseudonucleotide components are of the formula: (1) wherein each Y is independently O or S; each X is independently H, PO3-2, an activated nucleotide synthesis coupling moiety, a protecting group, a nucleoside, a nucleotide or a nucleotide sequence, or comprises a solid support; F is a functional group capable of linking an additional moiety or said group already reacted to effect the binding of said additional moiety; &squ& is an organic backbone which does not contain additional F or Y-X substituents and which is either achiral even when the Y-X substituents are different, or is a single enantiomer of a chiral compound; with the proviso that at least one X is a nucleoside, nucleotide, nucleotide sequence, an activated nucleotide synthesis coupling moiety, or comprises a solid support, or F represents said functional group already reacted with an additional group. Oligonucleotides having the pseudonucleoside at the 3' terminus are particularly stable in vivo.
摘要:Schmidberger, J. W.; Hepworth, L. J.; Green, A. P.; Flitsch, S. L., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 336. 摘要:Hollmann, F., Science of Synthesis Knowledge Updates, (2021) 3, 437. 摘要:Schafer, E. W., Jr., W. A. Bowles Jr., and J. Hurlbut. 1983. The acute oral toxicity and repellency and hazard potential of 998 chemicals to one or more species of wild and domestic birds. Archives of Environmental Contamination and Toxicology 12:355-382. 参考文献:10.1007/s10863-006-9007-4 摘要:McCarty RE. The Decay of the ATPase Activity of Light Plus Thiol-Activated Thylakoid Membranes in the Dark. Journal of Bioenergetics and Biomembranes. 2006 Feb;38(1):67–74. doi: 10.1007/s10863-006-9007-4.