- One-pot microwave-assisted selective azido reduction/tandem cyclization in condensed and solid phase with nickel boride
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An efficient and inexpensive method using microwave-assisted irradiation with Ni2B for the syntheses of aromatic amines, pyrrolobenzodiazepines as well as pyrroloquinazolinones was developed. This protocol was applied in the tandem resin-cleavage, azido reduction, and cyclization of compounds 3 and 5 that afforded substituted pyrrolo[2,1-c][1,4] benzodiazepines 4 and 6 in a one-pot manner. The microwave-assisted irradiation reactions enhanced yields with very short reaction times in contrast to the conventional thermal reactions. Georg Thieme Verlag Stuttgart.
- Shankaraiah, Nagula,Markandeya, Nagula,Espinoza-Moraga, Marlene,Arancibia, Claudia,Kamal, Ahmed,Santos, Leonardo Silva
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experimental part
p. 2163 - 2170
(2009/12/31)
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- An efficient selective reduction of aromatic azides to amines employing BF3·OEt2/NaI: Synthesis of pyrrolobenzodiazepines
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A selective and facile method for the reduction of aromatic azides to amines by employing borontrifluoride diethyl etherate and sodium iodide. This methodology has been applied towards the preparation of biologically important imine-containing pyrrolobenzodiazepines and their dilactams through intramolecular reductive-cyclization process. In this protocol the reagent systems are amenable for the generation of solution-phase combinatorial synthesis. Georg Thieme Verlag Stuttgart.
- Kamal, Ahmed,Shankaraiah,Markandeya,Reddy, Ch. Sanjeeva
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experimental part
p. 1297 - 1300
(2009/04/06)
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- ORGANIC COMPOUNDS
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The present invention relates to quinazolinone compounds of the formula wherein R2, R3, R5, R6 R7 and R8 are as defined in the specification and in the claims, in free form or in salt form , processes for their preparation and their use as pharmaceuticals, particularly in the treatment of disorders ameliorated by administration of TRPV1 antagonists.
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Page/Page column 61
(2008/06/13)
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- A mild and facile reduction of azides to amines by N,N-dimethylhydrazine and catalytic ferric chloride
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Reaction of a variety of azido compounds with N,N-dimethylhydrazine in the presence of a catalytic amount of ferric chloride hexahydrate in methanol results in excellent yields of the corresponding amino compounds. This reductive system is compatible with a wide assortment of functional groups and has also been extended towards the synthesis of pyrrolo[2,1-c][1,4]benzodiazepine antibiotics.
- Kamal, Ahmed,Reddy, B. S. Narayan
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p. 593 - 594
(2007/10/03)
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- Synthesis of pyrrolo[2,1-c][1,4]benzodiazepines via an intramolecular aza-Wittig reaction. Synthesis of the antibiotic DC-81
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A new and efficient synthesis of the pyrrolo[2,1-c][1,4]benzodiazepine ring system has been carried out using, as a key step, an intramolecular aza-Wittig reaction of the appropriately substituted N-(2-azidobenzoyl)pyrrolidine-2-carboxaldehydes. The paren
- Molina, Pedro,Diaz, Isidora,Tarraga, Alberto
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p. 5617 - 5630
(2007/10/02)
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