专利号:US-2003125243-A1 优先权日:2000-07-20 标题:Synthesis of cyclic peptides 发明人:LIU JUN; DAI XUEDONG; SU ZHUANG 摘要:The cyclic pentapeptide cyclo(-Arg-Gly-Asp-D-Phe-Lys-) is a highly potent and selective inhibitor for the α v β 3 integrin. A related compound, cyclo(-Arg-Gly-Asp-D-Phe-Val-), is a promising anticancer drug candidate; it has been found to inhibit angiogenesis and induce apoptosis in vascular cells. We have developed a synthesis of arginine containing cyclic peptides using the cyclizcation reagent 1-propanephosphonic acid cyclic anhydride (T3P) and the guanidine protecting group, 2,2,5,7,8-pentamethylchroman-6-sulfonyl (Pbf). This improved synthesis is environmentally friendly and is generally applicable to the synthesis of other cyclic peptides.
专利号:WO-2021108999-A1 优先权日:2019-12-03 标 题 :Method for continuous synthesis of 4-ethoxy-1,1,1-trifluoro-3-buten-2-one 发明人:HONG HAO; ZHANG ENXUAN; LU JIANGPING; SHEN WEI; YAN HONGLEI; LIU YUNPENG 权利人:LIAONING ASYMCHEM LABORATORIES CO LTD 摘要:Disclosed is a method for the continuous synthesis of 4-ethoxy-1,1,1-trifluoro-3-buten-2-one. The continuous synthesis method comprises: continuously introducing a raw material comprising vinyl ethyl ether, triethylamine and trifluoroacetic anhydride into a continuous reactor for a reaction to obtain a product system containing 4-ethoxy-1,1,1-trifluoro-3-buten-2-one, and continuously extracting the product system to obtain 4-ethoxy-1,1,1-trifluoro-3-buten-2-one. By using the continuous process, the above-mentioned raw materials can all be conveniently and accurately introduced into the continuous reactor, and after the reaction is completed, continuous extraction is also used for a post-treatment. The whole process is rapid, simple and efficient, the efficiency of the whole synthesis process is greatly increased, product destruction loss is reduced, and hidden safety hazards during batch production are avoided. After scaling up, there is no amplification effect, and safety and a relatively high synthesis efficiency can still be maintained.
专利号:US-6048975-A 优先权日:1991-09-12 标 题:Process for the chemical synthesis of oligonucleotides 发明人:PFLEIDERER WOLFGANG; BERGMANN FRANK 权利人:HOECHST AG 摘要:A process for the chemical synthesis of oligonucleotides n Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes. n The ease of detection of the dansyl protective group and the ease of elimination from the sugar residue of the nucleotide without side reactions make oligonucleotide synthesis possible with high yields in very small quantities.
专利号:US-9126995-B2 优先权日:2011-11-08 标题:Method for catalytic asymmetric synthesis of optically active isoxazoline compound and optically active isoxazoline compound 发明人:TOYAMA KEN-ICHI; MORIYAMA YUJI; MATOBA KAZUTAKA; YAOSAKA MANABU; IKEDA EITATSU 权利人:NISSAN CHEMICAL IND LTD 摘要:There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
专利号:WO-2011101864-A1 优先权日:2010-02-17 标题 :Novel process for the synthesis of phenoxyethyl derivatives 发明人:JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA 权利人:PANACEA BIOTEC LTD; JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA 摘要:The present invention provides an improved process for the synthesis of 2-[2- (2,2,2-trifluoroethoxy)phenoxy]ethanol intermediate, its derivatives and/or its pharmaceutically acceptable salts, useful in the synthesis of α-1 adrenoceptor blockers such as silodosin.
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.
摘要:Haynes, W.M. (ed.). CRC Handbook of Chemistry and Physics. 95th Edition. CRC Press LLC, Boca Raton: FL 2014-2015, p. 3-528 摘要:USEPA/Pollution Prevention and Toxics; 2012 Chemical Data Reporting Database. Ethane, 1,1,1-trifluoro- (420-46-2). Available from, as of Apr 4, 2016: 摘要:Pohanish, R.P. (ed). Sittig's Handbook of Toxic and Hazardous Chemical Carcinogens 6th Edition Volume 1: A-K,Volume 2: L-Z. William Andrew, Waltham, MA 2012, p. 2640 摘要:49 CFR 171.2 (USDOT); U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of February 10, 2016: 摘要:Haynes, W.M. (ed.). CRC Handbook of Chemistry and Physics. 95th Edition. CRC Press LLC, Boca Raton: FL 2014-2015, p. 6-144