- ANTIBACTERIAL COMPOUNDS
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This invention relates to antibacterial and antimycobacterial drug compounds of formula (I). It also relates to pharmaceutical formulations of antibacterial drug compounds of formula (I). It also relates to uses of the derivatives in treating bacterial infections and to methods of treating bacterial infections. The compounds are particularly useful for treating bacterial infections that have developed resistance to other drug compounds, e.g. resistant strains of S. aureus.
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Page/Page column 220
(2017/04/11)
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- Synthesis method of cis5-tert-butyl-3A-methyl-tetrahydro 1H-furan[3,4 c] pyrrole 3A,5(3H) dicarboxylic ester
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The invention relates to a synthesis method of cis5-tert-butyl-3A-methyl-tetrahydro 1H-furan[3,4 c] pyrrole 3A,5(3H) dicarboxylic ester. The method mainly solves the technical problem that no proper industrial synthesis method exists in the prior art. The method comprises five steps that: 1, a compound 1 uses sodium borohydride as a reducing agent to react in an ethanol solvent to obtain a compound 2; 2, the compound 2 uses tetrahydrofuran as a solvent to obtain a compound 3 under the effects of triphenylphosphine and diisopropyl azodicarboxylate; 3, the compound 3 and the N-methoxymethyl-N-(trimethylsilyl) benzylamine use dichloromethane as a solvent to obtain a compound 4 through room temperature reduction under the action of trifluoroacetic acid; 4, the compound 4 and thionyl chloride react under the methanol backflow condition to obtain a compound 5; 5, the compound 5 uses palladium hydroxide catalysts and Boc anhydride auxiliary agents to obtain a final compound 6 through catalytic hydrogenation reaction.
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Paragraph 0007
(2018/03/13)
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- MELANOCORTIN RECEPTOR AGONISTS
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The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.
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Page/Page column 30
(2008/06/13)
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- Asymmetric synthesis of the cis- And trans-stereoisomers of 4-aminopyrrolidine-3-carboxylic acid and 4-aminotetrahydrofuran-3-carboxylic acid
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The diastereoselective conjugate addition of lithium (S)-N-benzyl-N- α-methylbenzylamide has been successfully applied to the first asymmetric syntheses of cis-(3S,4R)- and fraBs-(3R,4R)-4-arninotetrahydrofuran-3-carboxylic acids (26% and 25% overall yield respectively, >98% d.e. and >97% e.e. in each case). Furthermore, the most efficient asymmetric synthesis to date of cis-(3R,4R)- and trans-(3R,4S)-4-aminopyrrolidine carboxylic acids is delineated: for cis-(3R,4R), four steps, >98% d.e., 52% overall yield; for trans-(3R,4S), five steps, >98% d.e., 50% overall yield.
- Bunnage, Mark E.,Davies, Stephen G.,Roberts, Paul M.,Smith, Andrew D.,Withey, Jonathan M.
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p. 2763 - 2776
(2007/10/03)
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