- An efficient and highly selective cleavage of N-tert- butoxycarbonyl group under microwave irradiation
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A simple and high yielding method for the cleavage of t-Boc carbamates is described which occurs under mild and solvent-free conditions using microwave irradiation.
- Bose, D. Subhas,Lakshmiriarayana
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- A practical method for the synthesis of highly enantioenriched trans -1,2-amino alcohols
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A highly enantioselective addition of phenyl carbamate to meso-epoxides has been developed to efficiently generate protected trans-1,2-amino alcohols. This transformation is promoted by an oligomeric (salen)Co-OTf catalyst and has been used to prepare two useful 2-aminocycloalkanol hydrochlorides in enantiopure form on a multigram scale from commercially available starting materials.
- Birrell, James A.,Jacobsen, Eric N.
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p. 2895 - 2897
(2013/07/26)
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- 6-O-SUBSTITUTED BENZOXAZOLE AND BENZOTHIAZOLE COMPOUNDS AND METHODS OF INHIBITING CSF-1R SIGNALING
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Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.
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Page/Page column 101
(2008/06/13)
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- CSF-1R INHIBITORS, COMPOSITIONS, AND METHODS OF USE
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Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.
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Page/Page column 82-83
(2009/01/20)
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- Stereocontrolled Preparation of Cyclohexane Amino Alcohols Utilising a Modified Mitsunobu Reaction
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A method for the introduction of amino groups into aliphatic systems is described.Cyclohex-2-enol reacts with aromatic diacylamines under Mitsunobu reaction conditions to give either N-alkylated or O-alkylated products in a controlled, predictable manner.
- Sammes, Peter G.,Thetford, Dean
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p. 655 - 661
(2007/10/02)
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- SYNTHESIS OF (L)-DAUNOSAMINE AND RELATED AMINO SUGARS
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1-(2-Furyl)ethanol (6) has been converted into methyl (+/-)-daunosaminide (1) and methyl (+/-)-ristosaminide (3) by use of an intramolecular cyclisation of a trichloroacetimidate group. (+/-)-Daunosamine (1) has been obtained more directly from the alcohol (10) by use of a modified Mitsunobu reaction; the scope of the latter reaction has been explored using cyclohex-2-en-1-ol as a model substrate.Asymmetric reduction of 2-acetylfuran (5) has given (S)-1-(2-furyl)ethanol (46) in good enantiomeric excess, thus providing a short route to the L-enantiomers of the amino sugars (1), (2), and (3) from a cheap, non-carbohydrate precursor.
- Sammes, Peter G.,Thetford, Dean
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p. 111 - 124
(2007/10/02)
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- NEW ROUTES TO CIS-1,2-HYDROXYAMINES AND RELATED SYSTEMS
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Use of modified Mitsunobu reactions followed by intramolecular cyclisations have been used to prepare cis-1,2-hydroxyamines, cis-1,3-hydroxyamines, 1,2,3-dihydroxyamines and 1,2,3-diaminoalcohols from allylic alcohols
- Sammes, Peter G.,Thetford, Dean
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p. 2275 - 2278
(2007/10/02)
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