105462-24-6Relevant articles and documents
A study on the synthesis of risedronic acid: The role of an ionic liquid additive
Nagy, Dávid Illés,Grün, Alajos,Sinkovicz, Júlia,Garadnay, Sándor,Greiner, István,Keglevich, Gy?rgy
, p. 238 - 244 (2019)
Background: The synthesis of high value risedronic acid is not fully resolved, as, for the time being, the best method based on the preparation from 3-pyridylcarboxylic acid by reaction with phosphorus trichloride in methanesulfonic acid gives risedronic acid in a good yield, but in an unpure form. Methods: Alternative protocols realizing the synthesis in sulfolane as the solvent and/or in the presence of suitable IL additive were developed to obtain the target dronic acid in a pure form. Results & Conclusion: Using phosphorus trichloride and phosphorous acid in two equivalents quantities together with 0.6 equivalents of [bmim][BF4] without any solvent, the method afforded the target dronic acid in a yield of 66% in a pure form.
An easy and effective method for synthesis and radiolabelling of risedronate as a model for bone imaging
Motaleb,Adli,El-Tawoosy,Sanad,Abdallah
, p. 157 - 163 (2016)
This study aimed to provide an easy method for synthesis of 1-hydroxy-2-(3-pyridyl) ethylidene bisphosphonic acid monosodium (sod. risedronate) with a high yield of 71%. The synthesized risedronate was labeled with technetium-99 m using two different reducing agents (SnCl2.2H2O and NaBH4) where NaBH4 gave stable complex and higher radiochemical yield more than SnCl2.2H2O. The results showed that, the radiochemical purity of 99mTc(NaBH4)-risedronate was 99.2 ± 0.6% and its stability was up to 6 h. Biodistribution study showed high uptake and long retention of 99mTc(NaBH4)-risedronate in bone starting from 15 min (29 ± 2.5% ID/organ) up to 4 h (35.1 ± 3.2 ID/organ) post injection. This research could introduce an easy and effective method for synthesis and labeling of risedrionate and affording a good tracer for bone imaging.
Environmentally friendly syntheses and tools
Keglevich, Gyoergy,Kovacs, Rita,Gruen, Alajos,Greiner, Istvan
, p. 39 - 41 (2013)
Recent results obtained by our group on MW-assisted reactions, such as the alkylation of PO-functionalized CH-acidic compounds and the addition of dialkyl phosphites to α-ketophosphonates, are summarized together with the rational synthesis of hydroxy-met
Preparation of (4-amino-1-hydroxybutylidene)bisphosphonic acid sodium salt, MK-217 (alendronate sodium). An improved procedure for the preparation of 1-hydroxy-1,1-bisphosphonic acids
Kieczykowski,Jobson,Melillo,Reinhold,Grenda,Shinkai
, p. 8310 - 8312 (1995)
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A method for preparing sodium
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Paragraph 0023; 0034; 0035, (2017/08/24)
The invention discloses a preparation method of risedronate sodium. The preparation method comprises the following steps of: (1) dissociating 3-pyridinecarboxylicacid chloride in 3-pyridinecarboxylicacid chloride hydrochloride; (2) reacting 3-pyridinecarboxylicacid chloride with diazomethane to generate a diazoketone compound represented by a formula (I); (3) generating 3-pyridylacetic acid under the common action of a catalyst and water; (4) adding hydrochloric acid, separating an organic phase from an inorganic phase, and evaporating and concentrating the inorganic phase to obtain 3-pyridylacetic acid hydrochloride; (5) converting 3-pyridylacetic acid hydrochloride into risedronic acid in the presence of phosphorus trichloride and phosphorous acid; and (6) reacting risedronic acid with sodium hydroxide solution to generate risedronate sodium. The preparation method of risedronate sodium disclosed by the invention has the advantages of being few in reaction step, short in reaction time, simple in post-treatment and higher in product yield.
