专利号:WO-2010103857-A1 优先权日:2009-03-12 标 题 :Method for solid-phase synthesis of glycopeptide using silicon-containing protecting group and synthesis device 发明人:NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN 权利人:UNIV HOKKAIDO NAT UNIV CORP; NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN 摘要:Disclosed are a novel method for the synthesis of a glycopeptide by which glycopeptides of various types can be deprotected and excised from a resin, each under weakly acidic to weakly basic conditions, without causing the problems of the epimerization of an amino acid at the a-position and the ß-elimination of a sugar residue; a synthesis device therefor; and a synthesis intermediate to be used in synthesizing a glycopeptide. Specifically disclosed are a method for the solid-phase synthesis of a glycopeptide which comprises a step for obtaining a glycopeptide derivative wherein the N-terminus is protected, the C-terminus is immobilized to a solid phase via a silicon linker, and a reactive group carried by a sugar residue and a reactive group carried by an amino acid side chain constituting a peptide are protected by silicon-containing groups, and a step for obtaining the glycopeptide by deprotecting said glycopeptide derivative and releasing the same from the solid phase by treating the glycopeptide derivative with an agent for removing the silicon-containing groups and the silicon linker; a synthesis intermediate to be used in the step for obtaining the glycopeptide derivative in the aforesaid method; and a device for the solid-phase synthesis of a glycopeptide.
专利号:US-8748660-B2 优先权日:2012-07-09 标题:Process for the synthesis of antiepileptic drug lacosamide 发明人:MURUGAN MUTHUKRISHNAN; MUJAHID MOHAMMAD; MAJUMDAR PRASHANT PRAMOD 权利人:MURUGAN MUTHUKRISHNAN; MUJAHID MOHAMMAD; MAJUMDAR PRASHANT PRAMOD; COUNCIL SCIENT IND RES 摘要:The present invention relates to the improved and efficient process for the synthesis of antiepileptic drug Lacosamide in high enantiopurity (>98% ee) and better yield. More particularly, the present invention relates to improved and efficient, cost effective process for synthesis of desired (R) isomer of Lacosamide starting from commercially available (S)-benzyl glycidyl ether.
专利号:WO-2024182268-A1 优先权日:2023-02-27 标 题 :Liquid phase peptide support synthesis of peptides and peptidomimetics 发明人:HAN AMY 权利人:REGENERON PHARMA 摘要:The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.
专利号:US-3978084-A 优先权日:1973-12-03 标题 :Synthesis of biotin 发明人:CONFALONE PASQUALE NICHOLAS; USKOKOVIC MILAN RADOJE; PIZZOLATO GIACOMO 权利人:HOFFMANN LA ROCHE 摘要:Synthesis of biotin from 4-carbomethoxy-2-(4,5-dihydrothiophen-3(2H)-one)-valeric acid methyl ester, and thiophene intermediates in this synthesis.
专利号:US-3979396-A 优先权日:1973-12-03 标 题 :Synthesis of biotin 发明人:CONFALONE PASQUALE NICHOLAS; USKOKOVIC MILAN RADOJE; PIZZOLATO GIACOMO 权利人:HOFFMANN LA ROCHE 摘要:Synthesis of biotin from 4-carbomethoxy-2-(4,5-dihydrothiophen-3(2H)-one)-valeric acid methyl ester, and dihydrothiophene intermediates in this synthesis.
专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
参考标题:Stereoselective Synthesis Of Medium-Sized Cyclic Ethers By Sequential Ring-Closing Metathesis And Tsuji-Trost Allylation 作者:James Skardon-Duncan,Michael Sparenberg,Alexandre Bayle,Sam Alexander,J. Stephen Clark |发布日期:2018.5.4 摘要:Fully Functionalized Medium-Sized Cyclic Ethers, Of The Type Found In Fused Polyether Natural Products, Have Been Prepared By Sequential Ring-Closing Diene Metathesis, Conversion Of The Resulting Cyclic Enone Into An Allylic Enol Carbonate, And Tsuji-Trost Allylation Using A Chiral Palladium Complex. Very High Levels Of Diastereocontrol, Favoring The Diastereomer In Which There Is A Cis Relationship
合成参考文献
摘要:Zimmer, R.; Trawny, D., Science of Synthesis Knowledge Updates, (2013) 4, 161. 摘要:Wessjohann, L. A.; Kaluđerović, G. N.; Neves Filho, R. A. W.; Morejon, M. C.; Lemanski, G.; Ziegler, T., Science of Synthesis: Multicomponent Reactions, (2013) 1, 445. 摘要:Currance, P.L. Clements, B., Bronstein, A.C. (Eds).; Emergency Care For Hazardous Materials Exposure. 3Rd edition, Elsevier Mosby, St. Louis, MO 2005, p. 176-7 摘要:Franke C et al; Chemosphere 29: 1501-14 (1994) 摘要:USEPA, Office of Prevention, Pesticides, and Toxic Substances; Interim Acute Exposure Guideline Levels (Aegls) for Selected Chloroformates (May 2008). Available from, as of July 31, 2012: https://www.epa.gov/oppt/aegl/pubs/chloroformates_interim.pdf