- TRACELESS REDUCTIVELY CLEAVABLE LINKER MOLECULES FOR PEPTIDE PURIFICATION
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The present invention relates to linker molecules of formula (1), X-Tb-Va-U-Y-Z (1) and a method for purifying peptides using said linker molecules. The linker molecule can be coupled to a purification resin via the moiety X and to a
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Page/Page column 73-74
(2020/03/23)
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- PYRAZOLE-OXAZOLIDINONE COMPOUND FOR ANTI-HEPATITIS B VIRUS
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The present invention discloses a pyrazole-oxazolidinone compound having anti-hepatitis B virus activity, which has the structure of formula (I), wherein each variable is as defined herein.
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Paragraph 0221-0224
(2019/06/07)
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- Preparation method for 5-fluoroindole-2-ketone
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The invention discloses a preparation method for 5-fluoroindole-2-ketone. The preparation method comprises the following steps: taking 2,4-difluoronitrobenzene as a raw material, enabling the 2,4-difluoronitrobenzene to perform condensation reaction with dimethyl malonate in an aprotic polar solvent under an inorganic alkaline condition, and performing post-treatment to obtain 4-fluoro-2-(dimehtylmalonate) nitrobenzene; in the presence of the aprotic polar solvent and lithium chloride, enabling the 4-fluoro-2-(dimehtyl malonate) nitrobenzene to generate 5-fluoro-2- nitrobenzene methyl acetate; mixing the 5-fluoro-2- nitrobenzene methyl acetate, a catalyst and alcohol solvents to perform hydrogenation cyclization reaction to obtain a 5-fluoroindole-ketone crude product; taking water as thesolvent by the crude product, filtering active carbon while hot, and re-crystallizing to obtain high-purity 5-fluoro-indole-2-ketone. The method adopts easily available raw materials, is simple in process; and a Raney nickel catalyst and a recrystallization aqueous solution can be used for many times, the raw material cost is relatively low, industrialization is easily realized, and the application prospect is relatively great.
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- BIS-ARYL COMPOUNDS FOR USE AS MEDICAMENTS
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There is provided compounds of formula I, wherein ring A, D1, D2a, D2b, D3, L1, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
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Page/Page column 85; 86
(2009/12/02)
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- A Convergent Synthesis of 14-Membered F-O-G Ring Analogs of the Teicoplanin Binding Pocket via Intramolecular SNAr Reaction
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An intramolecular SNAr reaction for efficient macrocyclization via biaryl ether formation was developed for syntheses of the 14-membered macrocycles 2 and 3 related to F-O-G ring of teicoplanin 1.Chloride as well as fluoride could be used as the leaving group in this reaction.However, the latter was prefered since it required milder conditions.Both ortho and para nitro, fluoro disubstituted aromatic rings were suitable for the macrocyclization reaction with tethered aryl oxides.The nonproteinogenic α-amino acid 23, required for the synthesis of 3, was prepared via an asymmetric Strecker synthesis using (R)-phenylglycinol as a chiral auxiliary.The overall synthetic strategy was convergent, and the cyclization could be performed in the presence of the highly sensitive arylglycine unit without racemization.
- Zhu, Jieping,Beugelmans, Rene,Bourdet, Sebastien,Chastanet, Jacqueline,Roussi, George
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p. 6389 - 6396
(2007/10/03)
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- A general oxindole synthesis
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A general synthesis of indol-2(3H)-ones (oxindoles), was developed based on the addition of dimethyl malonate to commercially available halonitrobenzenes. The advantage of this route over many other oxindole syntheses was the regiochemical control of the substitution pattern on the aromatic ring.
- Quallich,Morrissey
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