摘要:
The present invention provides substituted oxazolidinone derivatives, which can be used as antimicrobial agents. Compounds disclosed can be used for the treatment or prevention of a condition caused by or contributed to by bacteria, such as, inter alia, multiply-resistant Staphylococci, Streptococci, Enterococci, Bacterioides spp., Clostridium spp., Mycobacterium spp. Bacillus spp., Corynebacterium spp. Heptoslreptacoccus spp. Listeria spp., Legionella spp., Haemophilus influenza, Moraxella, Eschericia faecalis, and Eschericia coli. Processes for the preparation of disclosed compounds, pharmaceutical compositions thereof, and method of treating microbial infection are provided.
摘要:
The present invention relates to an improved process for the preparation of 5,6-dihydro-4-(S)-(ethylamino)-6-(S)methyl-4H-thieno[2,3b]thiopyran-2-sulphonamide-7,7-dioxide hydrochloride of formula (I) commonly known as Dorzolamide Hydrochloride useful as an agent to reduce intraoccular pressure by inhibiting carbonic anhydrase enzyme
摘要:
The present invention relates to a process for the in situ preparation of optically pure (S)-3,4-dihydroxybutyric acid derivatives represented by the Formula [2] and more particularly, to a process which enables preparing optically pure (S)-3-hydroxy-&ggr;-butyrolactone represented by Formula [1] by oxidation of &agr;- or &bgr;-(1,4) linked disaccharide or oligosaccharide with an oxidant under basic condition to give acid and cyclization sequentially under acidic condition to give (S)-3-hydroxy-&ggr;-butyrolactone.
摘要:
The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1 -butynyl)-tetrahydrofuran and precursors thereof.
摘要:
A process for the preparation of 1-[(cyano) aryl methyl] cyclohexanol of the general formula 1 (1a-d) by reacting cyclohexanone with the carbanions of an aryl acetonitrile of the general formula 3 (3a-d), a) R1=H, R2=H b) R1=OMe R2=H c) R1=OMe R2=OMe d) R1=OMe R2=cyclopentyloxy using a base, isolating the compound of formula 1 and purifying the compound of formula 1a-d by crystallisation is disclosed.
摘要翻译:通过使环己酮与通式3(3a-d)的芳基乙腈的碳阴离子反应制备通式1(1a-d)的1 - [(氰基)芳基甲基]环己醇的方法,a)R1 公开了通过结晶分离式1化合物和纯化式1a-d的化合物的方法,其中R 1 = OMe R 2 = OMc)R 1 = OMe R 2 =使用碱的环戊氧基。
摘要:
The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1-butynyl)-tetrahydrofuran and precursors thereof.
摘要:
The invention relates to novel dipyrano-quinolinone class of compounds having the general formula: Wherein R is hydrogen, alkyl optionally substituted about C-1 to C-10 alkenyl optionally substituted about C-1 to C-10 with one or more double bounds, alkynyl optionally substituted about C-1 to C-10 with one or more triple bonds, aryl, hetero aryl, carbocyclic aryl, alkyl aryl, alcyclic compounds, C-1 to C-6 alkyl with terminal dialkyl amino group, thio alkyl, hydroxyl alkyl groups; R1 is H, lower dialkyl amino alkyls such as methyl, ethyl, propyl, and other alkyl groups or b-amino acid moieties, hydroxy alkyl groups having optionally substituted about C-1 to C-10 carbons, acid amides such as aliphatic acids, aromatic acids, sulphonic acids trihalo acids. x—x is either a carbon-carbon single bond or a carbon-carbon double bond; R2 and R3, R4 and R5 are each independently hydrogen and methyl there by resulting the cis and trans diastereomers as well as enantiomers; R4 and R5 are each independently hydrogen and methyl while R6 and R7 are each independently hydrogen and hydroxyl/—OR8, where R8 is independently alkyl, aryl alkyl, amino alkyl, hydroxy alkyl with C-1 to C-10 carbons, sugars which include mono saccharides both in the furanose form as well as pyranose form, amino sugars, disaccharides, amino acids, small peptides through lower alkyl spacer groups, thereby resulting the cis and trans diastereomers as well as enantiomers; and a process for producing the above novel dipyrano-quinolinone class of compounds.
摘要:
The Present invention relates to a process for the preparation of (RS) 3-methyl-1-(2-piperidinyl phenyl) butyl amine of formula 1. (RS) 3-Methyl-1-(2-piperidinyl phenyl butyl amine having formula 1 is an important key intermediate for the synthesis of repaglinide of formula 2 an oral hypoglycemic agent.
摘要:
The invention provides new methods for preparation of cyclic oxygen compounds, including 2,5-disubstituted tetrahydrofurans, 2,6-disubstituted tetrahydropyrans, 2,7-disubstituted oxepanes and 2,8-oxocanes. The invention also provides new cyclic oxygen compounds and pharmaceutical compositions and therapeutic methods that comprise such compounds.
摘要:
The invention provides new methods for preparation of cyclic oxygen compounds, including 2,5-disubstituted tetrahydrofurans, 2,6-disubstituted tetrahydropyrans, 2,7-disubstituted oxepanes and 2,8-oxocanes. The invention also provides new cyclic oxygen compounds and pharmaceutical compositions and therapeutic methods that comprise such compounds.