- O-benzoylhydroxylamines as alkyl nitrene precursors: Synthesis of saturated N-heterocycles from primary amines
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We introduce O-benzoylhydroxylamines as competent alkyl nitrene precursors. The combination of readily available, stable substrates and a proficient rhodium catalyst provides a straightforward means for the construction of various pyrrolidine rings from the corresponding primary amines. Preliminary mechanistic investigation suggests that the structure of the nitrene precursor plays a role in determining the nature of the resulting reactive intermediate.
- Noda, Hidetoshi,Asada, Yasuko,Shibasaki, Masakatsu
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supporting information
p. 8769 - 8773
(2020/10/12)
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- Efficient oxidation of alcohols electrochemically mediated by azabicyclo-N-oxyls
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Preparation of azabicyclo-N-oxyls and the electrochemical oxidation of alcohols using them as mediators have been exploited. This oxidation was applicable to a transformation of sterically hindered secondary alcohols into the corresponding ketones in high yields.
- Demizu, Yosuke,Shiigi, Hirofumi,Oda, Takahisa,Matsumura, Yoshihiro,Onomura, Osamu
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- Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X1, X2, X3, X4, X5, R5, R6, R7, R8a, R8b, R9, Z1, Z2 and L are as defined in the description.
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- Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
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The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.
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- Novel amides useful for treating pain
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The present invention relates to compounds of formula (I-VII) or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R6, R7 and R8 are defined herein. The present invention also relates to methods of trating pain using these compounds and pharmaceutical compositions including these compounds.
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Page/Page column 28
(2010/02/11)
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- Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
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- Piperadinyl-substituted pyridylalkane, alkene and alkine carboxamides
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The invention relates to new piperidinyl-substituted pyridyl carboxamides of the general formula (I), wherein the structure element E has meanings (E1) or (E2) and whereby the heterocyclic ring can optionally have a double bond. These substances have especially high cytostatic activities and pronounced immunosuppressive properties which make them suitable for therapeutic treatment in broad tumor spectrum.
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- Synthetic Approaches to Nortropanes and Nortrop-6-enes; Intramolecular Displacement by Nitrogen in 7-Membered Rings
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The synthesis of simple nortropane and nortrop-6-ene derivatives from cyclohepta-1,3-diene is described.The key intermediates are trans-1-amino-4-chloro-cycloheptanes and -cyclohept-2-enes which are derived efficiently from the corresponding cis-amino-alcohols and undergo intramolecular cyclisation.Corresponding derivatisation of cyclohexa- and cycloocta-1,3-dienes is explored and attempts to achieve Pd-catalysed cyclisation of 1-amino-4-acetoxy-derivatives is described.Nitrogen inversion data for selected nortropane derivatives are included. Key Words: nortropanes/enes; 1,4-disubstitute cyclohexanes, cycloheptanes, cyclooctanes and -enes; intramolecular cyclisation; slow nitrogen inversion.
- Naylor, Antoinette,Howarth, Nicola,Malpass, John R.
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p. 451 - 468
(2007/10/02)
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- SPIRO-ISOXAZOLIDINE DERIVATIVES AS CHOLINERGIC AGENTS
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Compounds of general formula I, STR1 wherein: A represents (CH. sub.2) m optionally substituted by R 3,B represents (CH. sub.2) n optionally substituted by R 4, R. sub.1 represents hydrogen, C 1-C 6 alkyl, C 1-6 alkenyl or C 1-6 alkynyl, R 2 represents hydrogen, C 1-C 6 alkyl or COOR 5, in which R 5 represents C 1-C 6 alkyl,R 3 and R. sub.4 independently represent hydrogen or C 1-C 6 alkyl, in addition, any two of R. sub.2, R 3 and R 4 may together form a C 1-3 alkylene chain,n and m independently represent an integer from 1-3 inclusive,Y represents O or S,and pharmaceutically acceptable acid addition salts thereof are useful as pharmaceuticals, in particular as central muscarinic acetylcholine receptor agonists. The compounds are therefore useful in the treatment of diseases such as presenile and senile dementia, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania and Tourette Syndrome.
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- A SIMPLE APPROACH TO NORTROPANE AND NORTROP-6-ENE DERIVATES
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Intramolecular cyclisation of trans-1-(benzylamino)-4-chlorocycloheptane and hept-2-ene gives the corresponding 8-azabicyclo(3.2.1)octane (nortropane) and -oct-6-ene (nortrop-6-ene) derivatives respectively.Under appropriate conditions, cyclohept-1,3-diene is converted into nortropane in 75percent overall yield.
- Bathgate, Antoinette,Malpass, John R.
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p. 5937 - 5940
(2007/10/02)
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