专利号:EP-0310950-B1 优先权日:1983-11-18 标题 :Quinoline intermediates for the synthesis of 1H-imidazo[4,5-c]quinolines and 1H-imidazo[4,5-c]quinolin-4-amimes 摘要:Compounds of the types (I) and (II) are disclosed, wherein each R5 is independently selected from the group consisting of alkyl of one to about four carbon atoms, alkoxy of one to about four carbon atoms and halogen, and n is an integer from 0 to 2, with the proviso that if n is 2, then said R5 substituents together contain no more than 6 carbon atoms; R6 is selected from the group consisting of hydroxyalkyl of one to about six carbon atoms and cyclohexylmethyl; and R7 is selected from the group consisting of alkyl of one to about four carbon atoms and hydrogen. These compounds may be used as intermediates for the synthesis of 1H-imidazo[4,5-c]quinoline derivatives.
专利号:US-3558614-A 优先权日:1967-09-05 标题:Synthesis of tetranuclear dyes 发明人:JENKINS PHILIP W 权利人:EASTMAN KODAK CO 摘要:TETRANUCLEAR DYES DERIVED FROM A 2-IMIDAZOLIN-4-ONE, A 2-IMIDAZOLIN-4-THIONE AND A 2-IMIDAZOLIN-4-SELENONE ARE PREPARED IN GOOD YIELDS BY CONDENSING A QUATERNIZED MEROCYANINE DYE DERIVED FROM A 2-IMIDAZOLIN-4-ONE, A 2-IMIDAZOLIN-4-THIONE OR A 2-IMIDAZOLIN4-SELENONE WITH (1) A DIALKOXYALKYL ESTER OF AN ORGANIC ACID, (2) A TRIALKOXY ALKANE OR ARYL COMPOUND, (3) A 3,3-DIALKOZY-1ALKOXYPROPENE, (4) A 1-ANILINO-5-PHENYLIMINO-1,3-PENTADIENE OR (5) A SECOND QUATERNIZED MROCYANINE DYE DERIVED FROM A 2-IMIDAZOLIN-4-ONE, A 2-IMIDAZOLIN-4THIONE OR A 2-IMIDAZOLIN-4-SELENONE, EACH HAVING SUBSTITUTED ON THE CARBON IN THE 2-POSITION A GROUP SUCH AS A B-ACETANILIDOVINYL GROUP, A 4-ACETANILIDO-1,3-BUTADIENYL GROUP, AND A 6-ACETANILIDO-1,3,5-HEXADIENYL GROUP.
专利号:US-5688933-A 优先权日:1989-10-16 标题 :Preparation of biologically active compounds from substantially pure enantiomers of 2-azabicyclo 2.2.1!hept-5-en-one 发明人:EVANS CHRISTOPHER THOMAS; ROBERTS STANLEY MICAHEL 权利人:CHIROSCIENCE LTD 摘要:Lactams of 1-amino-3-carboxylic acid cyclic compounds are provided in enantiomeric form, together with an enantiomer of the corresponding ring-opened amino-acid or ester, by reaction of the racemic lactam with a novel lactamase. The products are useful in the synthesis of chiral carbocyclic nucleotides. The enantiomer is preferably 2-azabicyclo 2.2.1!hept-5-en-3-one.
专利号:US-4216319-A 优先权日:1976-06-09 标题:Synthesis of 2,4-diamino-5-benzylpyrimidines using benzyl cyanoacetal intermediates 发明人:SWARINGEN ROY A JR; YEOWELL DAVID A 权利人:BURROUGHS WELLCOME CO 摘要:Benzyl cyanoacetals of formula: ##STR1## wherein R 1 , R 2 and R 3 are the same or different and each is a halogen or a hydrogen atom, an alkoxy group, an alkyl group, or a dialkylamino group; R 4 is an alkoxycarbonyl group, or an aldehyde group; and R 5 is an alkyl group; the alkyl or alkoxy groups each having from 1 to 4 carbon atoms, and their use as intermediates in the preparation of antibacterial 2,4-diamino-5-benzylpyrimidines. They are prepared from a reaction between an orthoester and an α-substituted-β-benzylpropionitrile and then the resulting cyanoacetal is converted to the benzylpyrimidine by reaction with guanidine.
专利号:WO-2017222946-A1 优先权日:2016-06-20 标题 :Adenylyl cyclase inhibitors, pharmaceutical compositions and methods of use thereof 发明人:LEVY DANIEL E; ABARZUA PATRICIO; VATNER DOROTHY E; VATNER STEPHEN 权利人:VASADE BIOSCIENCES 摘要:Disclosed are inhibitors of adenylyl cyclase of Formula (I) having variables as described, as well as methods of synthesis thereof, pharmaceutical compositions thereof, and methods of treatment of various diseases using the pharmaceutical compositions.
专利号:US-5126347-A 优先权日:1989-02-13 标 题 :Isomeric dideoxynuclesides 发明人:HURYN DONNA M; TAM STEVE YIK-KAI; WEIGELE MANFRED 权利人:HOFFMANN LA ROCHE 摘要:Isomeric derivatives of 2',3'-dideoxyadenosine and 2',3'-dideoxyguanosine wherein the adenine or guanine base is attached to the 1' position of the iso-dideoxysugar residue by the 9-N position, the novel intermediates used in the synthesis of these compounds, and a method for treating a subject infected with a retrovirus by administering the compounds of the invention.
[参考文献]: M Cushman, Et Al. Synthesis Of 2,6-Dioxo-(1H,3H)-9-N-Ribitylpurine And 2,6-Dioxo-(1H,3H)-8-Aza-9-N-Ribitylpurine As Inhibitors Of Lumazine Synthase And Riboflavin Synthase. Bioorg Med Chem. 1998 Apr;6(4):409-15.
合成参考文献
摘要:Liang, Y.; Wen, Z.; Cabrera, M.; Howlader, A. H.; Wnuk, S. F., Science of Synthesis Knowledge Updates, (2020) 1, 206.