16179-41-2Relevant academic research and scientific papers
Voriconazole derivative, synthesis thereof, and use thereof in long-acting preparation
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Paragraph 0089, (2017/03/17)
The invention relates to a compound of formula (I), and a salt, an N-oxide, a quaternary ammonium and a stereoisomer thereof. R to R in the formula (I) are as defined in claims. The invention also relates to an intermediate for preparing the compound of formula (I), and a method for preparing the compound of formula (I). The invention further relates to a use of the compound of formula (I) as a drug especially used for preventing or treating fungal infection.
Fosaprepitant derivative, synthesis thereof, and use thereof in long acting preparation
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Paragraph 0082, (2017/04/03)
The invention relates to a Fosaprepitant derivative, a synthesis thereof, and a use thereof in a long acting preparation. The invention relates to a compound of formula (I), and a salt, an N-oxide, a quaternary ammonium and a stereoisomer thereof. R to R in the formula (I) are as defined in claims. The invention also relates to an intermediate for preparing the compound of formula (I), and a method for preparing the compound of formula (I). The invention further relates to a use of the compound of formula (I) as a drug especially used for preventing chemotherapy induced acute and late nausea and vomiting.
Posaconazole derivative, synthesis and application in prolonged action preparation thereof
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Paragraph 0087, (2017/04/03)
The invention relates to a posaconazole derivative, synthesis and an application in a prolonged action thereof. The invention relates to a formula of a compound and salt, N-oxide, quaternary ammonium and stereoisomer of the compound, wherein R1-R8 are defined according to what is claimed. The invention also relates to a preparation formula of an intermediate body and a method of the compound. The invention further relates to a formula of an application of the compound as a drug, especially the application in preventing or treating fungal infection. The detailed formulas are in the specification.
FOSFLUCONAZOLE DERIVATIVES, SYNTHESIS, AND USE IN LONG ACTING FORMULATIONS
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Page/Page column 25-27, (2010/10/03)
The invention relates to a compound of formula (I) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein R1 to R8 are as defined in the claims. The invention further relates to intermediates and methods for the preparation of the compounds of formula (I). The invention also relates to the compounds of formula (I) for use as a medicament, particularly for the prevention or treatment of fungal infections.
Combinatorial synthesis of PEG oligomer libraries
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Page/Page column 11, (2010/02/15)
A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.
PROCEDE DE PREPARATION DE COMPOSES ESTER UTILISES COMME ACTIVATEURS DE BLANCHIMENT
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Page/Page column 7-8, (2008/06/13)
La présente invention concerne un procédé de préparation de composé ester activateur de blanchiment. Ce procédé consiste (A) à préparer un monoester d'acide gras, (B) à fabriquer un chloroformate par réaction de ce monoester d'acide gras avec au moins un
Design, synthesis, and evaluation of water-soluble phospholipid analogues as inhibitors of phospholipase C from Bacillus cereus
Franklin, Christopher L.,Li, Hui,Martin, Stephen F.
, p. 7298 - 7307 (2007/10/03)
The rate of hydrolysis of natural phospholipids by the phosphatidyleholine-preferring phospholipase C from Bacillus cereus (PLC Bc) follows the order phosphatidylcholine > phosphatidylethanolamine ? phosphatidyl-L-serine. To probe the structural basis for this substrate specificity, a series of water-soluble, nonhydrolyzable substrate analogues were needed so their complexes with the enzyme could be studied via X-ray crystallography and isothermal titration calorimetry (ITC). Accordingly the water-soluble dithiophospholipids 2-10 having choline, ethanolamine, and L-serine headgroups were synthesized, and the inhibitory activity of each was determined in an assay using 1,2-dihexanoyl-sn-glycero-3-phosphocholine (C6PC) as the monomeric substrate. The 1,2-dibutanoyl dithiophosphocholine 2 was a weak inhibitor, whereas the related 1,2-dipentanoyl dithiophospho-choline 3 and the ethylene glycol dithiophosphocholines 4 and 5 were moderate inhibitors. The 1,2-ω -hydroxydiacyl dithiophosphocholines 6 and 7 were potent inhibitors, while the related compound 8, which had shorter acyl side chains, was a weak inhibitor. The dithiophosphoethanolamine 9 was a modest inhibitor, whereas the dithiophospho-L-serine 10 was a somewhat weaker inhibitor. Overall, the phospholipid analogues had increasing Ki values according to the order 2 ? 10 3 4 ≈ 5 ≈ 8 9 ? 6 ? 7 and increasing solubility according to the sequence 5 ≈ 7 4 ≈ 6 ≈ 9 3 10 8 2.
Oxidative ring cleavage of cyclic acetals with hypervalent tert-butylperoxy-λ3-iodanes
Sueda, Takuya,Fukuda, Sonoko,Ochiai, Masahito
, p. 2387 - 2390 (2007/10/03)
(matrix presented) Exposure of cyclic acetals to 1-tert-butylperoxy-1,2-benziodoxol-3(1H)-one in the presence of tert-butyl hydroperoxide and potassium carbonate in benzene at room temperature results in oxidative ring cleavage to glycol monoesters via intermediate tert-butylperoxy ortho esters.
Direct Oxidation of Acetals and Aldehydes to Esters
Takeda, Takanobu,Watanabe, Hidenori,Kitahara, Takeshi
, p. 1149 - 1150 (2007/10/03)
One step conversion of acetals and aldehydes to esters was achieved with hydrogen peroxide (35wt% solution in water) and hydrochloric acid in alcohol. This procedure was proved to be simple and effective.
Structure and origin of artifacts in the analysis of plasmalogens
Dudda, Angela,Spiteller, Gerhard
, p. 303 - 308 (2007/10/03)
The determination of aldehydic compounds was achieved by gas chromatographic/mass spectrometric analysis of derived thioacetals. These were produced, together with artifacts, in a one-step reaction when plasmalogens were treated with ethane-1,2-dithiol and BF3. The artifacts Were recognized to be 2-alkylidene-1,3-dithiolanes derived from phospholipids. The latter were converted by BP, treatment into diacylglycerols, which were transformed in a complicated reaction into 2-alkyl-2-((2-mercaptoethyl)thiol-1,3-dithiolane. These compounds were decomposed thermally, e.g. in the injector of a gas chromatograph, in 2-alkylidene-1,3-dithiolanes, This reaction is not restricted to phospholipids but occurs with all monoacylated glycols.
