- Synthesis method of 3-aminopyrrole-2-formamide compound
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The invention discloses a synthesis method of a 3-aminopyrrole-2-formamide compound. The synthesis method comprises the following steps of: 1) a compound is prepared by using ammonia or alkylamine R1NH2 and chloroacetamide as raw materials and water as a solvent under the condition of ice bath; 2) under the condition of ice bath, the compound and another compound are used as raw materials and react in the solvent under the action of sodium acetate to prepare a compound; and 3) the compound is used as the raw material and subjected to a ring closing reaction in the solvent under the action of alkali, and the target compound is obtained. The method has the advantages of short synthesis route, mild reaction conditions, few side reactions, simple post-treatment method, high yield and low cost,and is suitable for large-scale industrial production.
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Paragraph 0035-0037
(2020/11/05)
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- 1-METHYLCARBAPENEM DERIVATIVES
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The present invention relates to 1-methylcarbapenem compounds having excellent antibacterial activity, pharmacologically acceptable ester derivatives thereof, pharmacologically acceptable salts thereof, pharmaceutical compositions (particularly antibacterial agents) containing them as active ingredient, use of the compounds, ester derivatives or salts thereof for preparing such pharmaceutical compositions and a method of preventing or treating diseases (particularly bacterial infections) in which a pharmacologically effective amount of the compound, ester derivative or salt is administered to a warm-blooded animal (particularly a human being). The 1-methylcarbapenem compounds of the present invention are represented by the general formula (I): wherein:R1 is a group represented by the formula COOR3 (wherein R3 represents a hydrogen atom, a C1-C6 alkyl group or the like), a group represented by the formula CONR4R5 (wherein R4 and R5 each independently represent a hydrogen atom, a C1-C6 alkyl group which may be substituted or the like), a cyano group, a group represented by the formula CH2OR6 (wherein R6 represents a hydrogen atom, a C1-C6 alkyl group or the like) or a group represented by the formula CH2NR7R8 (wherein R7 represents a hydrogen atom, a C1-C6 alkyl group or the like, and R8 represents a hydrogen atom, a C1-C6 alkyl group, a C1-C6 alkanoyl group, a C1- C6 alkoxycarbonyl group or the like);R2 represents a hydrogen atom or a C1-C6 alkyl group;n represents 1, 2 or 3; andX represents a sulfur atom or an oxygen atom.
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- Prodrug derivatives of carboxylic acid drugs
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Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R1 and R2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R1 and R2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution. The novel derivatives are less irritating to mucosa than the parent carboxylic acids and may provide an improved bio-availability of the drugs.
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