- On the preparation of 4-hydroxymethyl-5-methyl-1,3-dioxol-2-one
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A practical and efficient conversion of 4-bromomethyl-5-methyl-1,3-dioxol-2-one 1 into the corresponding carbinol 2, a useful building block for the preparation of prodrugs, is reported.
- Alpegiani,Zarini,Perrone
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- MONOETHYLENICALLY UNSATURATED MONOMERS AND USES THEREOF
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The invention relates to a monoethylenically unsaturated monomer of formula (I), and to the use thereof for producing a polymer. The invention also relates to the polymer obtained by polymerising said monomer, and to the use thereof in a composition for producing coatings.
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- N-SUBSTITUTED-CYCLIC AMINO DERIVATIVE
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The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is -N(R1b)-, G2 is -CO-, G3 is -C(R1c)(R1d)-, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c, and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.
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Page/Page column 159
(2012/05/20)
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- Novel prodrugs for antimicrobial amidines
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A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): wherein: X may be O, S, or NR′ wherein R′ is H or loweralkyl; R1 and R2 may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R5 is represented by a formula selected from the group consisting of: ?wherein: X1, X2, and X3 are independently selected from O and S; and R6 and R7 are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.
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- A convenient method for the conversion of halides to alcohols
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The displacement of halides in unactivated primary bromides and iodides, allylic and benzylic primary and secondary bromides, and primary and secondary α-bromoketones by formate, using triethylammonium formate as the formylating agent, followed by acid or base catalyzed hydrolysis has been found to be an efficient method for the conversion of halides to alcohols.
- Alexander,Renyer,Veerapanane
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p. 3875 - 3881
(2007/10/03)
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- Dioxolenylmethyl carbamates pro moieties for amine drugs
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This invention relates to a the use of new oxodioxolenylmethyl carbamates to produce bioreversible neutral prodrugs from primary and secondary amines.
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