2-溴-6-甲氧基吡啶置于copper(I) Oxide,四甲基氯化铵,L-脯氨酸体系中,用 乙醇 用作溶剂,化学反应 24.0H,以70%的收率获得2-氯-6-甲氧基吡啶 参考文献:Copper-Catalyzed Conversion Of Aryl And Heteroaryl Bromides Into The Corresponding Chlorides 标题:Copper-Catalyzed Conversion Of Aryl And Heteroaryl Bromides Into The Corresponding Chlorides 摘要:描述了一种合成芳基和杂芳基氯化物的高效方法.在温和反应条件下,芳基和杂芳基溴化物与四甲基氨基氯化铵在铜催化剂存在下顺利反应,产生了相应的氯化物,产率令人满意至非常好. Doi:10.1039/c2Cc34944B
专利号:US-6271379-B1 优先权日:2000-03-08 标题:Intermediates useful for the synthesis of huperzine A 发明人:TUECKMANTEL WERNER; KOZIKOWSKI ALAN P 权利人:UNIV GEORGETOWN 摘要:Intermediates useful for the synthesis of huperzine A represented by the structures below, n and methods for their synthesis, wherein: n R 1 is lower alkyl, benzyl, or substituted benzyl; n X is a suitable leaving group; n Y is an electron withdrawing group that can subsequently be converted into an amino group; n one broken line is present as a carbon—carbon bond and the other broken line is absent, where the broken line forms an unconjugated carbon—carbon double bond, which double bond may be endocyclic whereby n is 3 or the double bond may be exocyclic whereby n is 2.
专利号:US-5428166-A 优先权日:1992-06-18 标 题 :Method of making asymmetric de ring intermediates for the synthesis of camptothecin and camptothecin analogs 发明人:COMINS DANIEL L 权利人:UNIV NORTH CAROLINA STATE 摘要:A method of making racemic DE ring intermediates for the synthesis of camptothecin and camptothecin analogs employing novel intermediates of Formula XX and XXI: ##STR1## as precursors to the DE ring intermediate. The present invention also provides camptothecin analog of Formula I-A ##STR2## wherein: Hal is a halogen is selected from the group consisting of F, Cl, and Br; n R may be loweralkyl; n R 1 may be H, loweralkyl, loweralkoxy, or halo; n R 2 , R 3 , R 4 , and R 5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkyl-thio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, amninomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom. n Additionally, novel compounds useful in the preparation of the compounds of Formula I-A are also provided.
专利号:US-9221821-B2 优先权日:2012-06-05 标题:Methods for the synthesis of 1,3-substituted aminouracils and other xanthine-related compounds 发明人:DIEP NHUT; KALYAN YURIY B 权利人:FOREST LAB HOLDINGS LTD; FOREST LAB HOLDINGS LTD 摘要:Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
专利号:US-5212317-A 优先权日:1990-12-20 标 题:Methods and intermediates for the assymmetric synthesis of camptothecin and camptothecin analogs 发明人:COMINS DANIEL L; BAEVSKY MATTHEW F 权利人:UNIV NORTH CAROLINA STATE 摘要:Processes for making compounds of Formulae XIV, XV, and XVII ##STR1## wherein R 6 is lower alkyl, R 7 is lower alkyl, R is lower alkyl, Y is H, F or Cl, R 8 is a moiety of Formula XVIII ##STR2## wherein n is 1, 2, or 3, R 11 is C 1 -C 4 alkyl and R 12 is the same as R 11 , or R 11 and R 12 together form cyclopentane or cyclohexane, and R 13 is: n (a) phenyl substituted 1 to 5 times with C 3 -C 7 secondary alkyl or C 4 -C 7 tertiary alkyl, or n (b) selected from the group consisting of naphthyl, anthryl, and phenanthryl optionally substituted 1 to 5 times with C 3 -C 7 secondary alkyl or C 4 -C 7 tertiary alkyl groups, n R 10 is C 6 -C 10 alkyl, aryl or alkyl aryl, n and Y is H, F or Cl, n are disclosed. These processes can be used to make optically enhanced and optically pure forms of the compounds, which are useful in the making of camptothecin and analogs thereof.
专利号:US-5258516-A 优先权日:1990-12-20 标题 :Optically pure D,E ring intermediates useful for the synthesis of camptothecin and camptothecin analogs 发明人:COMINS DANIEL L; BAEVSKY MATTHEW F 权利人:NC STATE UNIVERSITY 摘要:Processes for making compounds of Formulae XIV, XV, and XVII ##STR1## wherein R 6 is lower alkyl, R 7 is lower alkyl, R is lower alkyl, Y is H, F or Cl, R 8 is a compound of Formula XVIII ##STR2## wherein n is 1, 2, or 3, R 11 is C 1 -C 4 alkyl and R 12 is the same as R 11 , or R 11 and R 12 together form cyclopentane or cyclohexane, and R 13 is: n (a) phenyl substituted 1 to 5 times with C 3 -C 7 secondary alkyl or C 4 -C 7 ; tertiary alkyl, or n (b) selected from the group consisting of naphthyl, anthryl, and phenanthryl optionally substituted 1 to 5 times with C 3 -C 7 secondary alkyl or C 4 -C 7 tertiary alkyl groups, n R 10 is C 6 -C 10 alkyl, aryl or alkyl aryl, n and Y is H, F or Cl, n are disclosed. These processes can be used to make optically enhanced and optically pure forms of the compounds, which are useful in the making of camptothecin and analogs thereof.
专利号:US-8114993-B2 优先权日:2007-02-06 标题:Use of aryl chlorides in palladium-catalyzed C-H bond functionalization 发明人:DAUGULIS OLAFS; CHIONG HENDRICH 权利人:DAUGULIS OLAFS; CHIONG HENDRICH; UNIV HOUSTON SYSTEM 摘要:A one-step method for efficiently converting carbon-hydrogen bonds into carbon-carbon bonds using chloroarenes and palladium catalysts is disclosed. This method allows faster introduction of complex molecular entities, a process that would otherwise require many more steps. This invention is particularly relevant for the organic synthesis of complex molecules such as, but not limited to, pharmacophores.
[参考文献]: V Arjunan, Et Al. Density Functional Theory Studies On Vibrational And Electronic Spectra Of 2-Chloro-6-Methoxypyridine. Spectrochim Acta A Mol Biomol Spectrosc. 2011 May;78(5):1625-32.
合成参考文献
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