专利号:US-6624294-B2 优先权日:1999-01-08 标 题:Regioselective synthesis of 2′-O-modified nucleosides 发明人:KAWASAKI ANDREW M; FRASER ALLISTER S; MANOHARAN MUTHIAH; COOK P DAN; PRAKASH THAZHA P 权利人:ISIS PHARMACEUTICALS INC 摘要:Methods for the regioselective alkylation at the 2'-hydroxy position over the 3'-hydroxy position of nucleosides and nucleoside analogs, forming 2'-O-ester modified compounds, are disclosed. Reduction and derivatization of the 2'-O-ester provides 2'-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.
专利号:US-7485718-B2 优先权日:2005-06-16 标题:Chemical synthesis of low molecular weight polyglucosamines and polygalactosamines 发明人:SABESAN SUBRAMANIAM 权利人:DU PONT 摘要:A process for the synthesis of beta linked low molecular weight polymers of galactosamine and glucosamine has been developed. Through the use of high amounts of activating agents, efficient coupling of stable monomers is achieved. Using this process, chain extension is through the addition of single monomers, providing populations of single chain length polyhexosamines.
专利号:US-4987253-A 优先权日:1988-09-19 标 题 :Method for the synthesis of desferrioxamine B and analogs thereof 发明人:BERGERON RAYMOND J 权利人:UNIV FLORIDA 摘要:Disclosed is a synthesis of desferrioxamine B and analogs and homologs thereof beginning with the generation of the O-protected N-(4-cyanobutyl)hydroxylamine which is acylated at the O-benzylhydroxylamine nitrogen with either succinic or acetic anhydride. The resulting half-acid amide or amide respectively, is subjected to a series of high yield condensations and reductions which provide desferrioxamine B in 45% overall yield. Finally, a desamino analog of desferrioxamine is prepared in order to demonstrate the synthetic utility of the scheme as applied to desferrioxamine derivatives.
专利号:US-12129222-B2 优先权日:2016-08-11 标题:Production of bitter principle derivatives 发明人:WYRWA RALF; RODE CLAUDIA; SEEMANN THOMAS; MEINEL LORENZ; RITZER JENNIFER; SCHNABELRAUCH MATTHIAS 权利人:UNIV WUERZBURG J MAXIMILIANS; JULIUS MAXIMILIANS UNIV 摘要:It is an object of the present invention to introduce carboxylic acid-functionalities suitable for coupling into the denatonium structure by means of simple synthesis, namely the synthesis of bitter principle derivatives based on the denatonium structure according to formula 1:For example, according to the invention, lidocaine derivatives may be reacted with carboxylated benzyl halogenides. The carboxylated denatonium derivatives of the present invention are especially applied in medicine, biology, medical engineering as well as cosmetics, the pharmaceutical, chemical, and foodstuff industry.
专利号:US-10465033-B2 优先权日:2016-11-10 标题:One step synthesis of ultrahigh molecular weight block copolymers 发明人:URBAN MAREK W 权利人:UNIV CLEMSON; UNIV CLEMSON RES FOUNDATION 摘要:Single-step synthesis processes for production of ultrahigh molecular weight block copolymers are described. The ultrahigh molecular weight copolymers can have a molecular weight of about 10 6 or greater and can be formed within a few hours in a surfactant-free environment. The formation process is controlled by initiator-starvation conditions in a sequential polymerization of monomers exhibiting different solubility in the solvent.
专利号:US-2023391818-A1 优先权日:2020-11-05 标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation 发明人:NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.