专利号:US-7939679-B2 优先权日:2006-01-19 标题:Method for synthesis of ciguatoxin CTX1B and compounds useful for the synthesis of ciguatoxin CTX1B 发明人:HIRAMA MASAHIRO; INOUE MASAYUKI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:Disclosed is a method for total synthesis of CTX1B, which is developed for the synthesis of a ciguatoxin analogue such as CTX3C and enables the more efficient application of an established reaction to the total synthesis of CTC1B. More specifically, disclosed is a method for total synthesis of CTX1B comprising; an O.S-acetal formation for synthesizing a novel compound (3); a radical cyclization reaction for constructing a 9-membered ring formation reaction including a novel compound (6) through a novel compound (8) and yielding a compound (D); and a deprotection for yielding CTX1B. Also disclosed are novel compounds (1) to (8) which are particularly useful for synthesis of CTX1B and can be used for the synthesis of a ciguatoxin analogue.
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:WO-2022256490-A9 优先权日:2021-06-03 标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus 发明人:LOCKWOOD MARK 权利人:ANTIOS THERAPEUTICS INC 摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
专利号:US-2022267266-A1 优先权日:2019-07-09 标 题 :Improved, cost effective process for synthesis of vitamin d3 and its analogue calcifediol from ergosterol 发明人:DATLA ANUPAMA; NAGRE PRASHANT; TAMORE JAGDISH; PRABHU MANOJKUMAR SADANAND; KADAM SACHIN VASANT 权利人:FERMENTA BIOTECH LTD 摘要:Disclosed herein is an improved and efficient process for synthesis of vitamin D3 and its analogue Calcifediol from Ergosterol. Particularly, the present invention discloses the synthesis of key intermediate 3β-tert-Butyldimethylsilyloxy-22-hydroxy-23,24-bisnorchola-5,7-diene (5), and novel intermediate β-tert-Butyldimethylsilyloxy-22-iodo-23,24-bisnorchola-5,7-diene (9) by a simple and cost effective process. The industrially viable processes for preparation of said intermediate(s) results in providing provitamins with various side chains and the desired products in high yield.
专利号:US-11719709-B2 优先权日:2020-02-14 标题 :Water soluble polymer surfactant for synthesis of functionalized polystyrene nanobeads towards detection of bilirubin in human serum 发明人:MAKKAD SARABJOT KAUR; SYAMAKUMARI ASHA 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides a water soluble polymer surfactant (PS-DGlu) of formula I which is utilized for synthesis of functionalized polystyrene nanobead covalently incorporating (oligo) p-phenylenevinylene (OPV) nanosensor (PSG-OPV-n) which in turn is useful for the detection of bilirubin in human serum. The present invention further provides a process for the preparation of the water soluble polymer surfactant (PS-DGlu) of formula (I) and a mini emulsion polymerization process for the synthesis of PSG-OPV-n.wherein, n is 30-50.The PSG-OPV-n nanosensor beads show selectivity towards detection of bilirubin in presence of interferences such as glucose, sucrose, metal ions, cholesterol, and biliverdin with limit of detection of 20 nM. Ultimately, the invention also provides a kit for visual detection of bilirubin in human serum.
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.