- Method for preparation of alkyl phosphonyl compound from peroxide
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The invention discloses a method for preparation of an alkyl phosphonyl compound from peroxide. The invention adopts an acyl peroxide as the starting material, and the raw material is easily availableand has a great variety. The product obtained by the method provided by the invention has a great variety and wide uses. Some of the products can be reduced simply into important phosphorus ligands and key pharmaceutical intermediates. In addition, the method avoids the use of high toxicity phosphine reagent, has the characteristics of mild reaction conditions, simple operation, high target product yield, low pollution, simple reaction operation and post-treatment process, and is suitable for industrial production.
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Paragraph 0032; 0033
(2019/10/01)
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- Preparation method of alkyl phosphorylated substances
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The invention discloses a preparation method of alkyl phosphorylated substances. According to the invention, alkyl carboxylic acid is used as a starting material, and raw materials are easy to obtain and are various in types. Products prepared by the method disclosed by the invention are various in types and wide in application; and a part of the products can be prepared into important phosphorus ligands and drug key intermediates through simple reduction. In addition, use of high-toxicity phosphine reagents is avoided in the method, the reaction conditions are mild, operation is simple, the yield of the target product is high, pollution is small, and the reaction operation and post-treatment processes are simple, so that the method is suitable for industrial production.
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Paragraph 0024-0025
(2019/10/04)
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- A novel approach to phosphonic acids from hypophosphorous acid
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A novel access to phosphonic acids via Pd-catalyzed tandem carbon-phosphorus bond formation-oxidation processes was developed. The procedures involve atom-economical and environmentally friendly functionalization reactions of hypophosphorous acid (H3PO2) and H-phosphinic acids [RP(O)(OH)(H)].
- Bravo-Altamirano, Karla,Montchamp, Jean-Luc
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p. 5755 - 5759
(2008/02/09)
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- Selection of solid dosage form composition through drug-excipient compatibility testing
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A drug-excipient compatibility screening model was developed by which potential stability problems due to interactions of drug substances with excipients in solid dosage forms can be predicted. The model involved storing drug-excipient blends with 20% added water in closed glass vials at 50 °C and analyzing them after 1 and 3 weeks for chemical and physical stability. The total weight of drug-excipient blend in a vial was usually kept at about 200 mg. The amount of drug substance in a blend was determined on the basis of the expected drug-to-excipient ratio in the final formulation. Potential roles of several key factors, such as the chemical nature of the excipient, drug-to-excipient ratio, moisture, microenvironmental pH of the drug- excipient mixture, temperature, and light, on dosage form stability could be identified by using the model. Certain physical changes, such as polymorphic conversion or change from crystalline to amorphous form, that could occur in drug-excipient mixtures were also studied. Selection of dosage form composition by using this model at the outset of a drug development program would lead to reduction of 'surprise' problems during long-term stability testing of drug products.
- Serajuddin, Abu T. M.,Thakur, Ajit B.,Ghoshal, Rabin N.,Fakes, Michael G.,Ranadive, Sunanda A.,Morris, Kenneth R.,Varia, Sailesh A.
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p. 696 - 704
(2007/10/03)
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- Process for preparing phosphonic acids
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A process for preparing phosphonic acids of the structure STR1 wherein R1 is lower alkyl, aryl, cycloalkyl or arylalkyl, and R2 is H, benzyl or STR2 by oxidizing the corresponding phosphonous acid STR3 employing as the oxidizing agent potassium permanganate or sodium periodate.
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- PHOSPHONYL HYDROXYACYL AMINO ACID DERIVATIVES AS ANTIHYPERTENSIVE
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Phosphonyl hydroxyacyl amino acids of the formula STR1 wherein X is a substituted or unsubstituted imino or amino acid or ester. These compounds possess angiotensin converting enzyme activity and are thus useful as hypotensive agents.
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- PHOSPHONYL HYDROXYACYL AMINO ACID DERIVATIVES AS ANTIHYPERTENSIVES
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Phosphonyl hydroxyacyl amino acids of the formula STR1 wherein X is a substituted or unsubstituted imino or amino acid or ester. These compounds possess angiotensin converting enzyme activity and are thus useful as hypotensive agents.
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- PHOSPHONYL HYDROXYACYL AMINO ACID DERIVATIVES AS ANTIHYPERTENSIVES
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Phosphonyl hydroxyacyl amino acids of the formula STR1 wherein X is a substituted or unsubstituted imino or amino acid or ester. These compounds possess angiotensin converting enzyme activity and are thus useful as hypotensive agents.
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- Monophosphonate compounds as hypoglycemic and/or antiartherogenic agents
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This invention relates to new monophosphonate compounds of formula X--C6 H4 --(O)m --(CH2)n --R where R is --PO3 Me2, --PO3 Et2, --PO3 H2/s
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