专利号:WO-2024185734-A1 优先权日:2023-03-03 标 题:Polyphosphorylated nucleoside, phosphate-activated nucleotide used for synthesis of polyphosphorylated nucleoside and method for synthesis of same, and method for synthesis of polyphosphorylated nucleoside using phosphate-activated nucleotide 发明人:KATAOKA MASANORI; FUKUI CHIHARU; TSUJI YOHEI; FUJIMURA Kazuma 权利人:NATIAS INC 摘要:The present invention provides: a polyphosphorylated nucleoside which has a structure represented by formula (I) and can be efficiently produced by a short process and a simple operation with use of a less expensive material; a phosphate-activated nucleotide which is used for the synthesis of the polyphosphorylated nucleoside and a method for the synthesis of this phosphate-activated nucleotide; and a method for the synthesis of a polyphosphorylated nucleoside using a phosphate-activated nucleotide. In the formula, B represents a protected or unprotected, natural or artificial nucleoside base; R 1 , R 2 , R 4 and R 5 each represent H or an alkyl group or the like, and R 1 , R 2 , R 4 and R 5 may be the same as or different from each other; X and Y each represents H, OH, OCH 3 or the like; h represents an integer of 1 to 3; p, n, m and q each represent 0 or an integer, and p, n, m and q are in no particular order; and (p + n + m + q) is an integer of 0 to 5,000.
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-7692016-B2 优先权日:2005-11-25 标 题 :Process for the synthesis of quinoline derivatives 发明人:MADUGULA SREE RAMA MURTY; THALLAPELLY SWAMY; BANDARUPALLY JYOTHIRMAI; YADAV JHILLU SINGH 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides an improved process for the synthesis of quinoline derivatives. More particularly the present invention provides an improved and economical process for the synthesis of quinoline derivatives by the reaction of aniline/substituted anilines using two different catalysts, ferric chloride and zinc chloride in a one-pot set up reaction.
专利号:US-2025205370-A1 优先权日:2022-03-19 标 题:Synthesis of toluidine blue o and a kit for mucosal application 发明人:PANDA SWAGATIKA 权利人:PANDA SWAGATIKA 摘要:The present invention describes synthesis of Toluidine blue O for a formulation to be used for screening and biopsy site identification in oral cancer. The invention discloses two formulations and a method of delivery of the said formulations via a kit. The method described is a reproducible method of synthesis of pharmaceutical grade Toluidine blue O of acceptable purity and good colorimetric value. The present invention also discloses a kit that includes one formulation of a cleaning solution containing an organic acid and another formulation that is a vital stain formulation. The kit is packaged as a dual chamber sprayer having two pump dispensers, that facilitates ready to use, convenient dental chair side delivery, and allows mass screening.
专利号:US-10011580-B2 优先权日:2016-04-21 标题:Diastereoselective synthesis of (±)-epianastrephin, (±)-anastrephin and analogs thereof 发明人:WALSE SPENCER S; KUZMICH DANIEL 权利人:US AGRICULTURE 摘要:A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R 1 is ethenyl, R 2 and R 3 is methyl, and n is 1), (±)-anastrephin (2) (wherein: R 2 is ethenyl, R 1 and R 3 is methyl and n is 1), and analogs thereof (wherein: R 1 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 2 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 1 and R 2 together with the carbon atom they are attached form a C 3-6 cycloalkyl ring, R 3 is C 1-5 alkyl and n is 0-2):
专利号:US-4459420-A 优先权日:1982-05-17 标题 :Pyrogallol synthesis of anti-atherogenic furochromones 发明人:GAMMILL RONALD B 权利人:UPJOHN CO 摘要:The present invention provides a total synthesis of known intermediates useful in the synthesis of khellin and antiatherosclerotic analogs thereof from pyrogallol. Pyrogallol is converted to 3,6,7-benzofurantriol triacetate using zinc chloride and chloracetanitrile, then catalytically reduced and deactoxylated at the 3 position to yield the corresponding 2,3-dihydrofuran. This substance is subjected to a Fries rearrangement to the corresponding diol, the phenolic hydroxyl group of which is then selectively alkylated. This yields 6-hydroxy-7-alkoxy-5-benzofuranyl methyl ketone, a known intermediate for the production of 4-desmethoxy khellin and analogs thereof. This compound is then selectively alkoxylated at the 4 position using lead tetraacetate or thallium (III) nitrate in an alkanol solvent to yield known chemical intermediates in the preparation of khellin and analogs thereof.
参考标题:Synthesis Of 4-Ketocyclopentene And Cyclopentadiene Compounds 摘要:A Process For Forming 4-Ketocyclopentene And Substituted 4-Ketocyclopentene Compounds Starting From The Corresponding 1-Carbohydrocarbyloxy-2-Keto-4-Hydroxy-5-Cyclopentene By Reduction Followed By Decarboxylation Using Zinc Dichloride Or Zinc Dibromide. The Ketone May Thereafter Be Converted To A Cyclopentadiene Compound By Reducing The Ketone To Form An Alcohol, Replacing The Hydroxyl Functionality Of The Alcohol Under Substitution Conditions With A Leaving Group, And Deprotonating The Resulting Product Under Base Induced Elimination Conditions To Form The Cyclopentadiene Compound. Alternatively Functionalized Cyclopentadienyl Compounds Can Be Produced Without Isolation Of An Unsubstituted Cyclopentadienyl Compound By Combining The Elimination And Deprotonation Steps With A Replacement Step In A Single Unit Operation.
合成参考文献
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