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-8415510-B2 优先权日:2008-02-28 标题 :Synthesis of a PEG-6 moiety from commercial low-cost chemicals 发明人:ENGELL TORGRIM 权利人:ENGELL TORGRIM; GE HEALTHCARE LTD 摘要:The present invention provides novel synthesis's for obtaining a protecting group aminoxy PEG-6 linker from cost effective, and readily available starting materials and chemicals or modified polyethylene glycols. More specifically, a novel synthesis of obtaining a modified Boc-protected aminoxy PEG-6 linker was achieved so that said linker may be attached to a vector such as a peptide based fragment.
专利号:US-8536375-B2 优先权日:2008-12-22 标题:Synthesis of obtaining modified polyethylene glycol intermediates 发明人:ENGELL TORGRIM 权利人:ENGELL TORGRIM; GE HEALTHCARE LTD 摘要:The present invention provides novel and more efficient synthesis's for obtaining an intermediate in the synthesis of obtaining a protecting group aminoxy PEG linker.
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-6632942-B2 优先权日:2000-05-04 标题:Asymmetric synthesis of piperazic acid and derivatives thereof 发明人:ROBIDOUX ANDREA L C; SERAFINI SIRO; DIETERICH PETRA; LEONARDI STEFANIA; STIBBARD JOHN 权利人:VERTEX PHARMA 摘要:This invention provides a concise, asymmetric synthesis of piperazic acid and derivatives thereof, whereby either the (3S)- or (3R)-enantiomeric form may be obtained with high optical purity. (3S)-piperazic acid is derived from D-glutamic acid through an (R)-2,5-dihydroxyvalerate ester intermediate. After the hydroxy groups are converted to suitable leaving groups, such as mesylates, the ester is treated with a bis-protected hydrazine to provide the desired (3S)-piperazic acid derivative. The (3R) enantiomer of piperazic acid may be similarly obtained starting with L-glutamic acid. The method may also be used to obtain piperazic acid derivatives that have moderate optical purity or are racemic. By this method, piperazic acid derivatives may be obtained that are useful as intermediates for pharmacologically active compounds. For example, certain intermediates of this invention are useful for preparing caspase inhibitors, particularly inhibitors of ICE, through additional steps known in the art.
专利号:US-5679773-A 优先权日:1995-01-17 标题 :Reagants and methods for immobilized polymer synthesis and display 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:Compounds and methods for solid phase synthesis of organic molecules including peptides, oligonucleotides, benzodiazepines, beta -turn mimetics, and prostaglandins. The present invention provides new reagents in the form of linking groups and resins and substrates having attached linking groups which are useful in solid phase synthesis of high density arrays of organic molecules. The invention also provides methods which increase yields of various organic synthesis strategies.
[参考文献]: I H Hall, Et Al. Effects Of 2,3-Dihydrophthalazine-1,4-Dione On Sprague Dawley Rats Lipid Metabolism And Serum Lipoproteins. Biomed Biochim Acta. 1988;47(4-5):423-33. [参考文献]: I H Hall, Et Al. The Anti-Neoplastic Activity Of 2,3-Dihydrophthalazine-1,4-Dione And N-Butyl-2,3-Dihydrophthalazine-1,4-Dione In Human And Murine Tumor Cells. Anticancer Drugs. 1992 Feb;3(1):55-62. [参考文献]: J Schiller, Et Al. Differences In The Reactivity Of Phthalic Hydrazide And Luminol With Hydroxyl Radicals. Free Radic Res. 1999 Jan;30(1):45-57. [参考文献]: L Butner, Et Al. Anti-Inflammatory Activity Of 2,3-Dihydrophthalazine-1,4-Diones In Cf1 Mice. Int J Tissue React. 1996;18(2-3):47-55.
合成参考文献
摘要:Shaabani, A.; Sarvary, A.; Shaabani, S., Science of Synthesis: Multicomponent Reactions, (2013) 2, 103. 摘要:Li, J. J., Science of Synthesis: Knowledge Updates, (2025) 2. 参考文献:10.1007/s10529-014-1547-9 摘要:Zhang J, Chen S, Tan X, Zhong X, Yuan D, Cheng Y. Highly sensitive electrochemiluminescence biosensors for cholesterol detection based on mesoporous magnetic core-shell microspheres. Biotechnol Lett. 2014 Sep;36(9):1835–41. doi: 10.1007/s10529-014-1547-9. 参考文献:10.1021/la0609266 摘要:Mourran A, Ziener U, Möller M, Suarez M, Lehn JM. Homo- and heteroassemblies of lactim/lactam recognition patterns on highly ordered pyrolytic graphite: An STM investigation. Langmuir. 2006 Aug 29;22(18):7579–86. doi: 10.1021/la0609266.