N,N-Dimethylcarbamoyl-Phenylsulfone置于水体系中,用 四氢呋喃 作为反应溶剂,化学反应生成 苯磺酸 参考文献:Optimization Of Hno Production From N,O-Bis-Acylated Hydroxylamine Derivatives 标题:Optimization Of Hno Production From N,O-Bis-Acylated Hydroxylamine Derivatives 摘要:A Wide Range Of N,O-Bis-Acylated Hydroxylamine Derivatives With Chloro Or Arenesulfonyl Leaving Groups,And A Related Set Of N-Hydroxy-N-Acylsulfonamides,Have Been Synthesized And Evaluated For Nitroxyl (Hno) Production. Mechanistic Studies Have Revealed That The Observed Aqueous Chemistry Is More Complicated Than Originally Anticipated,And Have Been Used To Develop A New Series Of Efficient Hno Precursors (4U-4X,7C-7D) With Tunable Half-Lives. DOI:10.1021/ol203016C
专利号:US-5760237-A 优先权日:1995-08-25 标 题 :Synthesis of l-azatyrosine using pseudoephedrine as a chiral auxiliary 发明人:MYERS ANDREW G 权利人:CALIFORNIA INST OF TECHN 摘要:A practical synthesis of the potential chemotherapeutic agent L-azatyrosine is described. The key step involved the alkylation of (R,R)-(-)-pseudoephedrine glycinamide with 5-benzenesulfonyloxy-2-iodomethylpyridine and proceeded in 70-95% yield and 89-95% de. Simultaneous hydrolysis of the auxiliary and the benzenesulfonate protecting group afforded L-azatyrosine of ≧99% ee in 73% yield on multigram scale (recovery yield of (R,R)-(-)-pseudoephedrine: 90%).
专利号:WO-2013138200-A1 优先权日:2012-03-13 标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof 发明人:FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER 权利人:UNIV HOWARD 摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.
专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
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-7928223-B2 优先权日:2008-06-20 标题:Process for the synthesis of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:LERESTIF JEAN-MICHEL; LECOUVE JEAN-PIERRE; BRIGOT DANIEL 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n n n n n n n n n n Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-2004152905-A1 优先权日:2003-01-31 标题:Universal building blocks and support media for synthesis of oligonucleotides and their analogs 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and chemically modified oligonucleotide analogs, are provided. In addition, methods for functionalization of a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
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