- A new 1,2,3-triazolo[1,2]benzodiazepine ring system
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Dianion 2 derived from N-Boc-aminobenzotriazole 1 condenses in a [1.2]fashion with α,β-unsaturated aldehydes; subsequent oxidation of the resulting allylic alcohols 7 using manganese(IV) oxide or, less effectively, treatment of the derived acetates 10 with Pd(0), results in direct formation of the novel triazolo[1,2]-benzodiazepines 9 and 11 by intramolecular addition of the pendant amino group.
- Knight, David W.,Little, Paul B.
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- 1-Aminobenzotriazole functionalisation using directed metallation: New routes to chromanes and chromenes using intramolecular benzyne trapping by alcohols
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Metallation of 1-(tert-butoxycarbonylamino)benzotriazole 8 leads to the dianionic species 9 which undergoes smooth reactions with a range of electrophiles, under appropriate conditions. The derived iodide 30 undergoes efficient Sonogashira coupling with a range of alk-1-yn-3-ols to provide the expected arylalkynes 33, total or partial reduction of which leads to the arylpropanols 34 and the (Z)-allylic alcohols 40 respectively. N-Deprotection and exposure to N-iodosuccinimide then led to smooth benzyne generation and intramolecular trapping by the hydroxy functions with iodine incorporation to give the iodochromanes 35 and iodochromenes 41 respectively, in respectable overall yields. The Royal Society of Chemistry 2000.
- Knight, David W.,Little, Paul B.
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- NEW SUBSTITUTED BIPHENYL ANALOGUES AS DUAL INHIBITORS OF AROMATASE AND SULFATASE
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Provided are new biphenyl derivatives of formula (Ia). These compounds act as aromatase and sulfatase inhibitors. They are particularly useful for treating pathological conditions or diseases in which aromatase and sulfatase are involved. Moreover, provided are processes for the preparation of these compounds and pharmaceutical compositions containing said products and their use for the preparation of a medicament, in particular for the treatment of diseases characterized by aromatase and sulfatase activity such as hormone-dependent cancers.
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(2015/07/16)
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- 3-substituted cephem compounds
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The present invention relates to novel cephalosporins of the formula (I); STR1 wherein, R1 represents a C1 ?C4 alkyl group or STR2 wherein, R2 and R3, independently, represent hydrogen or a C1 ?C3 alkyl group and R4 represents hydrogen or a C1 ?C4 alkyl group; R1a represents hydrogen or an amino-protecting group; Q represents CH or N; and the formula STR3 represents a saturated or unsaturated heterocyclic group which contains 1 to 4 nitrogen atoms of which one is substituted with an amino group to form quaternary ammonium, and oxygen or sulfur, or a fused heterocyclic group thereof formed together with a substituted or unsubstituted benzene or an optional heterocyclic group, or a pharmaceutically acceptable salt thereof, to processes for preparing the same and to a pharmaceutical composition containing the same as an active ingredient. The compounds(1) according to the invention exhibit potent antibacterial activity and broad antibacterial spectrum against the Gram-positive strains including Staphylococcus as well as Gram-negative strains including Pseudomonas, and, therefore, are expected to be very useful in treatment of various diseases caused by bacterial infection in human beings and animals.
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