- Introduction of a polar functional group to the lipid tail of 4-epi-jaspine B affects sphingosine kinase isoform selectivity
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Sphingosine kinases (SphKs) are key enzymes that regulate sphingosine 1-phosphate production levels, and are involved in a range of cellular processes. Focusing on a hydrophilic residue in the hydrophobic binding pocket of SphKs, we designed and synthesiz
- Inuki, Shinsuke,Miyagawa, Takashi,Oishi, Shinya,Ohno, Hiroaki
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Read Online
- Method for Producing Amines from Hydroxamic Acids
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A method for producing unprotected or carbamate-protected amines of formulae (II) and (III) or R1—NH2 (II) or R1—NHCO2R2 (III) by reacting hydroxamic acids of formula (I) (R1CONHOH) with a) alkylphosphonic acid anhydrite's, b) alcohol R2OH and c) optionally with a base, at a temperature ranging from 100 to +120° C., wherein the hydroxamic acid (I) is produced prior to or during reacting (in situ) and R1 is an optionally substituted linear or branched C1-C12 alkyl radical, substituted C3-C10 cycloalkyl, alkenyl, aryl or heteroaryl radical and R2 is an open-chain, cyclic or branched allyl, aryl or C1 to C12-alkyl radicals, or aryloxy, allyloxy or alkoxy radical possibly substituted with open-chain, cyclic or branched C1 to C12-alkyl radicals.
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Page/Page column 3
(2008/12/08)
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- N-carboalkoxy-2-nitrobenzenesulfonamides: A practical preparation of N- Boc-, N-Alloc-, and N-Cbz-protected primary amines
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N-Carboalkoxy-2-nitrobenzenesulfonamides, readily prepared by acylation of 2-nitrobenzenesulfonamide (o-NsNH2), can be alkylated by either conventional or Mitsunobu protocols. Since the o-nosyl group can be deprotected under mild conditions, a variety of N-carboalkoxy derivatives of primary amines may be prepared in excellent yields from the corresponding alcohols and/or halides. In addition, allyloxycarbonyl (Alloc), t- butoxycarbonyl (t-Boc), and benzyloxycarbonyl (Cbz) groups can be deprotected in the presence of the o-nosyl group, allowing the resultant N-alkylated 2- nitrobenzenesulfonamides to be used for further preparation of secondary amines.
- Fukuyama, Tohru,Cheung, Mui,Kan, Toshiyuki
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p. 1301 - 1303
(2007/10/03)
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