- Synthesis, properties, and perspectives of gem-diphosphono substituted-thiazoles
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A series of substituted arylidene thiazoles were allowed to react with Wittig-Horner (WH) reagent, tetraethyl methyl-1,1-bisphosphonate, to produce via Michael addition reaction the corresponding heteroarylmethylenebisphosphonates (BPs) in different yields according to the experimental conditions. Acid hydrolysis of the new BPs was undertaken to obtain the corresponding bisphosphonic acids. Prediction and the in vivo activity of the products in the rat adjuvant model are also discussed in terms of structure-activity relationships (SAR).
- Abdou, Wafaa M.,Ganoub, Neven A.,Geronikaki, Athina,Sabry, Eman
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p. 1015 - 1024
(2008/09/20)
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- Synthesis of a new type of 1,1-bisphosphonates bearing S-, and N-heterocycles, based on the reactions of methylenebisphosphonate with alkenes
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The heterocycle-substituted 1,1-bisphosphonates 3a,b, 7, 10a,b and 12a,b were synthesized from the parent alkylidene substrates 2a,b, 6, 8a,b and 11a,b and methylenebisphosphonate 1 by a Michael addition reaction in different yields. Hydrolysis of 1,1-bisphosphonate product 3a with concentrated hydrochloric acid produced the corresponding 1,1-bisphosphonic acid 13.
- Abdou, Wafaa M.,Ganoub, Neven A. F.,El-Khoshnieh, Yehia O.
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p. 785 - 790
(2007/10/03)
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