990-91-0Relevant articles and documents
COMPOSITIONS AND METHODS FOR DETECTION OF TRAUMATIC BRAIN INJURY
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, (2021/12/03)
The present disclosure relates generally to compositions and methods for determining whether a patient suffers from a traumatic brain injury (TBI) by detecting the presence of an amyloid beta protein in an eye of the patient. Also provided are compositions and methods for preparing a patient for diagnosis and treatment of traumatic brain injury (TB).
A process for the preparation of [3 - [(2 R) - [(1 R) - 1 - [3, 5 - di (trifluoromethyl) phenyl] ethoxy] - 3 (S)- (4 - fluorophenyl) morpholine - 4 - yl] methyl] - 5 - oxo - 4, 5 - dihydro - [1, 2, 4] - triazole - 1 - yl] phosphine acid animal pen ester new method
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Paragraph 0049-0051, (2017/08/26)
The invention relates to a new method for preparing fosaprepitant intermediate, namely, [3-[(2R)-[(1R)-1-(3, 5-bi (trifluoromethyl) phenyl] ethyoxyl]-3 (S)-(4-fluorophenyl) morpholine 4-group] methyl]-5-oxo-4, 5-dihydro-[1, 2, 4]-triazole-1-group] phosphonic acid-benzyl ester. The compound is an important medicine intermediate, and is used for preparing antiemetic drug fosaprepitant. The new method comprises the steps of: enabling newly prepared phosphorylation agent dibenzyl phosphorus oxychloride and aprepitant to have reaction in organic solvent under the action of steric hindrance alkali, treating the product with methyl alcohol to obtain the fosaprepitant intermediate. The method is simple in operation and low in cost, thus being more suitable for industrial production.
A oxazolidinone compounds of preparation method (by machine translation)
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Paragraph 0042; 0043, (2017/05/12)
The invention provides a oxazolidinone compounds of the preparation method. Specifically provides the type 1 compound preparation method. The formula 1 compound preparation method comprises, formula 2 N - methyl - D - grape amine compound in the presence of a catalytic reduction, direct formula 1 compound. The present invention provides a preparation has simplified the reaction step, shorten the reaction route, can make the final yield of the product is higher, and, better purity. (by machine translation)
Selective P-P and P-O-P bond formations through copper-catalyzed aerobic oxidative dehydrogenative couplings of H-phosphonates
Zhou, Yongbo,Yin, Shuangfeng,Gao, Yuxing,Zhao, Yufen,Goto, Midori,Han, Li-Biao
supporting information; experimental part, p. 6852 - 6855 (2010/12/19)
(Chemical Equation Presented) Different copper complexes selectively catalyze the aerobic oxidative coupling of H-phosphonates to afford either hypophosphates and pyrophosphates in high yields with high selectivity (see scheme; tmeda = N, N, N', N'-tetramethylethylenediamine).
PROCESS FOR [3-[3(R)-[(R)-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]HOXY]-3(S)-(4-FLUOROPHENYL)MORPHOLIN-4-YL-5-OxO-4,5-DIHYDRO-[1,2,4]-TRIAZOL-1-YL PHOSPHONIC ACID
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Page/Page column 5, (2008/06/13)
The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(tri-fluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.
INDOLE COMPOUNDS USEFUL AS SEROTONIN SELECTIVE AGENTS
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Page/Page column 42, (2010/11/08)
Novel indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.
Reaction of chlorides of phosphoric, sulfonic, and carboxylic acids on solid potassium carbonate surface under PTC circumstances
Jaszay, Zsuzsa M.,Petnehazy, Imre,Toe, Laszlo
, p. 447 - 450 (2007/10/03)
Simple syntheses of phosphoric (4) and carboxylic (6) acid anhydrides have been elaborated by means of solid potassium carbonate in phase-transfer catalytic acylation. Behavior of various acid chlorides, phosphoric (1), sulfonic (2), and carboxylic (8), have also been studied toward potassium carbonate in the presence of lipophilic quaternary ammonium salt.
Thiosugar nucleotide analogs: Synthesis of 5′-(2,3,4-tri-O-acetyl-6-S-acetyl-6-thio-α-D-galactopyranosyl diphosphate)
Elhalabi, Jordan,Rice, Kevin G.
, p. 1935 - 1940 (2007/10/03)
The synthesis of a novel analog of uridine diphosphate galactose (UDP-Gal) is described. A sulfur atom was inserted into the 6-position of galactose to give uridine 5′-(2,3,4-tri-O-acetyl-6-S-acetyl-6-thio-α-D-galactopyranosyl diphosphate). This peracetylated thiol analogue of UDP-Gal has been synthesized in nine steps starting from methyl α-D-galactopyranoside in an overall yield of 3%.
Selective phosphorylation on primary alcohols of unprotected polyols
Ladame, Sylvain,Claustre, Samantha,Willson, Michele
, p. 37 - 47 (2007/10/03)
The triad tribenzylphosphite-iodine-pyridine offers a general selective method for phosphorylation reactions of primary alcohols of unprotected α-diols and polyols. A mechanistic study by 31P NMR allowed to evidence the formation, from iododibenzyl phosphate and pyridine, of a very reactive pyridinium salt intermediate. This analysis shows that pyridine behaves as a covalent catalyst like DMAP in acylation reactions from acylchloride. Due to its steric hindrance and high reactivity, this species appears to be the efficient selective phosphorylation reagent but leads to dibenzylphosphoric esters. Under mild conditions, the cleavage of benzyl groups gives monoester phosphoric acid.
