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The development of bisphosphonates for therapeutic uses, and bisphosphonate structure-activity consideration
Recent progress in the synthesis of major constituents of the methyl-1,1-bisphosphonate family is reviewed. These compounds are important precursors of the corresponding bisphosphonic acid with, inExpand
Symmetrical and Asymmetrical Bisphosphonate Esters. Synthesis, Selective Hydrolysis, and Isomerization
Summary.Two simple and efficient one-pot procedures for the synthesis of a series of α-branched N-heterocycle-substituted methane-1,1-bisphosphonates are outlined. In the first method, the parentExpand
An efficient method has been developed for the synthesis of phosphono substituted-heterocycles and vinylphosphonates. The procedure involves coupling reactions between α,α-dihalo-, α-monohalo- andExpand
Synthesis of Tetrazoloquinoline‐Based Mono‐ and Bisphosphonate Esters as Potent Anti‐Inflammatory Agents
Several new α-alkoxy- and α-hydroxyphosphonate derivatives of tetrazole-quinolines were synthesized from the reaction of 2-azidoquinolines 3-carboxaldehyde 1a,b with trialkyl phosphites and dialkylExpand
Use of phosphonyl carbanions in the synthesis of anti-inflammatory active phosphorus-containing fused heterocycles and relevance phosphonates.
The reaction of Horner-Emmons reactant carbanions with 2-acetyl-5-methyl furan 1 and 2-acetyl-5-bromothiophene 9 resulted in phosphorus-containing fused bicyclic 5,5-membered and 5,6-membered systemsExpand
Regioselective Condensation of Alkylidenephosphoranes with Bifunctionalized Compounds: New Approach to the Synthesis of Fused O- and N-Heterocycles
A series of fused pyran- (∼ 40% yield) and furan- (∼ 20% yield) derivatives were regioselectively prepared from the reactions of 5,6-difur-2′yl-3-oxo-2,3-dihydropyridazin-4-carbonitrile with ester-Expand
Antimicrobial activity of novel fused nitrogen, sulfur and phosphorus containing-heterocycles and relevant phosphonates with difurylpyridazine species
Treatment of 5,6-di(2-furyl)-3-thioxo-2,3-dihydropyridazine-4-carbonitrile with phosphonate carboanions stabilised with electron withdrawing group (CO2R, CN, SR’) led, under microwave irradiation andExpand
Synthesis, Quantitative Structure–Activity Relationship, and Anti-Inflammatory Profiles of Substituted 5- and 6-N-Heterocycle Bisphosphonate Esters
Abstract A modified multicomponent reaction in a one-pot synthesis of a new series of substituted N-heterocyclic aminomethylene bisphosphonates, in high rates, was described. Accordingly, synthesisExpand
A new conjugated addition of trialkyl phosphites and alkylidenephosphoranes to 3‐ω‐azideoacetyl coumarin synthesis of some 1,2,3,4‐triazaphospholes, triazoles, and azido‐coumarin derivatives
A new and efficient conjugate addition of trimethyl and triethyl phosphites to 3-ω-azidoacetylcoumarin (1) has been studied. The reaction proceeded smoothly at r.t. furnishing 1,2,3,4-triazaphospholeExpand