Classifications

• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
  • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
  • C07D498/18—Bridged systems
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
  • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
  • C07D513/18—Bridged systems

Definitions

• each X' is independently H or a functional group for coupling the synthon to at least a second bridged macrocyclic module or to a substrate
• each J is an independently selected functional group for coupling the synthon to an adjacent synthon within said bridged macrocyclic module
• each X ⁇ is an independently selected functional group which may couple the synthon to the bridge moiety
• R° is H, alkyl, or a lipophilic group; wherein R' is a natural ⁇ -amino acid side
• bridged macrocyclic module compounds may be found in the Examples and Claims.
• coupling of these reactive substituted linkages may be initiated by other chemical, thermal, photochemical, electrochemical, and inadiative methods to provide a variety of coupled structures.
• Each module may have 1 to 30 or more functional groups which may couple to a linker molecule.
• Linker molecules may have 1 to 20 or more functional groups which may couple to, for example, a module.
• a linker molecule has at least two functional groups, each of which can couple to a module and/or other component.
• linker molecules may include a variety of functional groups for coupling modules and/or other components. Non-limiting examples of functional groups of modules and linker molecules are illustrated in Table 8. Table 8: Examples of functional groups of modules and linker molecules
• linkers are found in the Examples. [0133] Methods of initiating coupling of the components to linker molecules include chemical, thermal, photochemical, electrochemical, and inadiative methods. [0134] Other methods for linking the components will be apparent to one of skill in the art.
• Scheme 4 illustrates an example of a general scheme for preparing bridged program director compounds.
• R is -CH 2 CO 2 (CH 2 ) 15 CH 3 .
• Example 39 e» ⁇ / ⁇ -Bicyclo[2.2.1]hept-5-ene-2-benzylcarboxylate-3-carboxyIic acid (S25-37) [0330]
• Compound S23-19 (4.00 g, 0.0244 mol) and quinidine (8.63 g, 0.0266 mol) were suspended in equal amounts of toluene (50 mL) and carbon tetrachloride (50 mL). The suspension was cooled to -55° C after which benzyl alcohol (7.90 g, 0.0732 mol) was added over 15 minutes. The reaction mixture became homogenous after 3 hours and was stined at -55° C for an additional 96 hours.
• Example 50 enrfo-Bicyclo[2.2.1]hept-5-ene-2-(4-methoxy)benzyl-3-(trimethylsilylethoxy- carbony ⁇ )amino carboxylate (S26-49) [0343] To a solution of S26-48 in benzene is added triethylamine and diphenylphosphoryl azide. The solution is refluxed for 24 hours, cooled to room temperature, trimethylsilylethanol is added, and the solution is refluxed for an additional 48 hours. The benzene solution is partitioned between ethyl acetate and 1 M sodium bicarbonate. The organic layers are combined, washed with 1 M sodium bicarbonate, and dried with sodium sulfate. The solvent is evaporated under reduced pressure to give crude Curtius product S26-49.

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• 2004
  • 2004-08-06 EP EP04809537A patent/EP1667965A2/en not_active Withdrawn
  • 2004-08-06 US US10/913,634 patent/US7368564B2/en active Active
  • 2004-08-06 WO PCT/US2004/025334 patent/WO2005030711A2/en active Application Filing
• 2008
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• 2012
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