- MANUFACTURING METHOD OF SODIUM FOSPHENYTOIN HYDRATE AND SYNTHETIC INTERMEDIATE THEREOF
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PROBLEM TO BE SOLVED: To provide a manufacturing method of sodium fosphenytoin hydrate capable of shortening time for all manufacturing processes and reducing manufacturing cost and a synthetic intermediate thereof. SOLUTION: There is provided a method for manufacturing 3-hydroxymethyl-5,5-diphenyl-2,4-imidazolidinedione, including a process for heating 5,5-diphenyl-2,4-imidazolidinedione (phenytoin), formaldehyde and alcohol and using no alkaline material. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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- Novel synthesis of fosphenytoin: Anti-convulsant prodrug
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A simple, new synthesis of fosphenytoin sodium 1, a prodrug, via imidate ester and employing mild reaction conditions is described. Copyright Taylor & Francis Group, LLC.
- Elati, Chandrashekar R.,Gangula, Srinivas,Naredla, Anitha,Ashok,Bhattacharya, Apurba,Bandichhor, Rakeshwarar
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p. 2950 - 2957
(2008/12/22)
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- PROCESS FOR PREPARING FOSPHENYTOIN
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Processes for preparing fosphenytoin.
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Page/Page column 14
(2010/11/28)
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- Process for the preparation of sodium fosphenytoin
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Phosphoric acid diester 2,5-dioxo-4,4-diphenylimidazolidin-1-ylmethyl esters, both of whose ester groups can be selectively cleaved, are obtained by converting 3-(hydroxymethyl)-5,5-diphenylimidazolidine-2,4-dione to an alkylsulfonate or arylsulfonate and reacting this with a phosphoric acid diester whose ester groups can be selectively cleaved from the reaction product. The two ester groups can be selectively cleaved from the phosphoric acid diesters obtained and the resulting product can be converted to 5,5-diphenyl-3-[(phosphonooxy)methyl]imidazolidine-2,4-dione disodium salt. The latter is an anticonvulsive, antiepileptic and antiarrhythmic known under the abbreviated name of sodium fosphenytoin.
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Page/Page column 3
(2008/06/13)
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- Phenytoin prodrugs III: Water-soluble prodrugs for oral and/or parenteral use
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Various bioreversible derivatives of phenytoin, a poorly water soluble and erratically absorbed drug after both oral and parenteral dosing, were synthesized. Initial evaluation of these expected prodrugs, i.e., their aqueous solubility, cleavage in the presence of various animal tissues, and anticonvulsant activity in mice, confirmed that a number of the derivatives did indeed behave as prodrugs. The more promising prodrugs were the disodium phosphate ester and various amino groups containing acyl esters of 3-(hydroxymethyl)-5,5-diphenylhydantoin.
- Varia,Schuller,Sloan,Stella
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p. 1068 - 1073
(2007/10/02)
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- Derivatives of 5,5-diphenylhydantoin exhibiting enhanced solubility and the therapeutic use thereof
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Novel derivatives of 5,5-diphenylhydantoin, having the formula: STR1 wherein R is as defined in the specification and claims hereinafter, are disclosed. These compounds exhibit enhanced solubility over diphenylhydantoin per se and find therapeutic usefulness as anticonvulsants, antiepileptics and antiarrhythmics.
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