- Use of oligosalicylates in the preparation of phenolic amido acids
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A simplified methodology has been developed for preparing salicylamides from the corresponding acids via oligosalicylates which both protect the phenolic group and, at the same time, activate the carboxyl for coupling. Copyright Taylor & Francis, Inc.
- Gschneidner, David,Corvino, JoAnne,Freeman, John,O'Toole, Doris,Shields, Lynn,Wang, Eric
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Read Online
- Development and in Vitro and in Vivo evaluation of microspheres containing sodium N-[8-(2-hydroxybenzoyl)amino]caprylate for the oral delivery of berberine hydrochloride
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Microspheres containing absorption enhancer (sodium N-[8-(2-hydroxybenzoyl) amino]caprylate, SNAC) were developed to enhance the oral bioavailability of berberine hydrochloride (BER) with poor intestinal membrane permeability. Microspheres were prepared a
- Li, Ying,Zhu, Chunyan
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Read Online
- Synthesis method of sodium N-(8-[2-hydroxybenzoyl]-amino)caprylate
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The present invention discloses a method for synthesizing N- (8-[2-hydroxybenzoyl]- amino) sodium caprylate. First, methyl o-hydroxybenzoate was added to the reaction vessel, and then a solvent and 8-aminocaprylic acid were added to the reaction; after th
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Paragraph 0027; 0030-0033; 0035-0038; 0040-0043
(2022/01/08)
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- Preparation method of N-(8-[2-hydroxybenzoyl]-amino) sodium caprylate and intermediate thereof
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The invention discloses a preparation method of N-(8-[2-hydroxybenzoyl]-amino) sodium caprylate and an intermediate thereof, and the preparation method of the intermediate comprises the following steps: reacting salicylamide with a protecting group reagen
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Paragraph 0076; 0082-0083; 0086; 0091-0092; 0095; 0100-0101
(2021/06/06)
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- Method for preparing N-[8-(2-hydroxybenzoyl)amino]caprylic acid
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The invention provides a method for preparing N-[8-(2-hydroxybenzoyl)amino]caprylic acid. The method is characterized in that salicylamide is used as an initial raw material and subjected to four-step reactions including cyclization, two-step nucleophilic substitution, hydrolysis and decarboxylation to obtain the N-[8-(2-hydroxybenzoyl)amino]caprylic acid. The preparation method has the advantages of easily available raw materials, low production cost, less three-waste pollution, simple process route and easy industrial production, and solves the problems that existing preparation methods are complex, raw materials are not easily available, requirements on equipment are low, and impurities are easily generated.
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Paragraph 0042; 0058-0061; 0062; 0077-0078
(2021/07/01)
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- Sodium 8-(2-hydroxylbenzamido)caprylate and preparation method therefor
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The invention discloses sodium 8-(2-hydroxylbenzamido)caprylate and a preparation method therefor and belongs to the field of preparation of compounds. A key of the technical scheme of the invention is as follows: the preparation method comprises the step
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- Preparation method of sodium 8-[(2-hydroxybenzoyl) amino] octanoate
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The invention discloses a preparation method of a pharmaceutical intermediate, i.e., sodium 8-[(2-hydroxybenzoyl) amino] octanoate. The preparation method comprises the steps of enabling salicylamide,used as a raw material, to react with N' N-carbonyl dii
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- METHOD OF TREATING VITAMIN B12 DEFICIENCY
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A method and composition for treating vitamin B12 deficiency in mammals that fail to respond to oral vitamin B12 therapy, including preparing a pharmaceutical composition for oral administration containing vitamin B12 and at least one substance selected f
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Page/Page column 6
(2009/06/27)
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- METHODS FOR PRODUCING N-(8-[2-HYDROXYBENZOYL]-AMINO) CAPRYLIC ACID
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Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hy
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Page/Page column 4-5
(2008/06/13)
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- Compounds and compositions for delivering active agents
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The present invention provides a compound having the formula or a salt thereof which facilitates the delivery of active agents. Compositions and dosage unit forms comprising the compound of the present invention and at least one active agent, such as a peptide, mucopolysaccharide, carbohydrate, or a lipid, are also provided. Methods of administration and preparation of the compounds and compositions of the invention are provided as well.
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Page column 29 - 30
(2008/06/13)
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- Method of preparing alkylated salicylamides
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The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide (hereinafter referred to as a “protected/activated salicylamide”). The method comprises the steps of (a) alkylating the protected/
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- Studies directed at the use of a parallel synthesis matrix to increase throughput in an in vivo assay
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Heparin is the anticoagulant of choice for hospitalized patients, but it is dosed only by injection because it is not absorbed following oral administration. We have discovered and prepared compounds (delivery agents) that facilitate the gastrointestinal absorption of heparin in rats, monkeys, and humans when given orally. We are currently developing a parallel synthesis approach to increase our delivery agent screening throughput in vivo. This approach has been used to produce micromolar quantities of compounds for testing in rats in a 5 x 5 parallel synthesis array. Using an amine benzoylation reaction sequence, 10 mixtures were prepared. These mixtures contained equal weight quantities of five N-substituted, non-α, amino acid delivery agents. Each of these mixtures was orally administered to rats in combination with heparin, and plasma clotting times (APTT) were measured to determine activity. Deconvolution of the data accurately identified the most active individual components. Independent synthesis of these compounds verified their activity. This parallel synthesis approach is an effective tool for the screening of oral heparin delivery agents and has increased screening throughput significantly.
- Leone-Bay,Freeman,O'Toole,Rosario-Gray,Salo-Kostmayer,Tai,Mercogliano,Baughman
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p. 3573 - 3576
(2007/10/03)
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- Method of preparing salicyloylamino acids
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A method for preparing salicyloylamino acids is provided. An oligosalicylate and an amino acid are reacted to yield the salicyloylamino acid.
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- Synthesis and evaluation of compounds that facilitate the gastrointestinal absorption of heparin
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A family of novel compounds (delivery agents) that promote the gastrointestinal absorption of USP heparin in rats and primates has been discovered. The delivery agents in combination with heparin were administered either orally or intracolonically in an aqueous propylene glycol solution and caused dramatic increases in both plasma heparin concentrations (anti-Factor Xa) and clotting times (APTT). Using one of the most effective delivery agents in this series, an estimated relative bioavailability of 8% can be achieved following oral administration to cynomolgus monkeys. To establish a correlation between the in vivo data and an in vitro parameter, immobilized artificial membrane (IAM) chromatography was performed. Log relative k' values were correlated to the efficiency of oral heparin delivery.
- Leone-Bay, Andrea,Paton, Duncan R.,Freeman, John,Lercara, Christine,O'Toole, Doris,Gschneidner, David,Wang, Eric,Harris, Elizabeth,Rosado, Connie,Rivera, Theresa,DeVincent, Aldonna,Tai, Monica,Mercogliano, Frank,Agarwal, Rajesh,Leipold, Harry,Baughman, Robert A.
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p. 1163 - 1171
(2007/10/03)
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