156816-78-3Relevant articles and documents
Racemic recovery method of by-product in resolution mother liquor of intermediate of sitafloxacin
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Paragraph 0040; 0041, (2019/01/07)
The invention discloses a racemic recovery method of the by-product in a resolution mother liquor of an intermediate of sitafloxacin. The method specifically comprises following steps: (1) carrying out resolution on a raceme 2-fluorocyclopropanecarboxylic
Novel 2-fluorocyclopropane carboxylic acid synthesis method
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Paragraph 0079; 0080, (2017/08/27)
The invention discloses a novel 2-fluorocyclopropane carboxylic acid synthesis method. The novel 2-fluorocyclopropane carboxylic acid synthesis method comprises the following steps: 1) enabling 1,1-dichloro-1-fluoroethane and thiophenol to react under the action of alkali to produce a phenyl sulfide intermediate; 2) implementing an oxidizing reaction between the phenyl sulfide intermediate and Oxone; 3) implementing an elimination reaction on an obtained product under the action of alkali to obtain 1-fluorine-1-phenylsulfonyl ethane; 4) implementing an addition reaction on the 1-fluorine-1-phenylsulfonyl ethane and ethyl diazoacetate under the action of a catalyst to obtain a cyclopropane intermediate; 5) implementing an elimination reaction on the cyclopropane intermediate under the action of alkali, and then acidifying to obtain 2-fluorocyclopropane carboxylic acid. The synthetic route is short, the materials are bulk commodities, cheap and easy to get, the Oxone replaces a commonly used mCPBA agent, the process is safely amplified, the reaction yield is increased, the production cost is greatly lowered, and the operation is simple.
Process for producing cyclopropanecarboxylates
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, (2008/06/13)
There is disclosed a process process for producing a cyclopropanecarboxylate of formula (1): 1which process comprises reacting cyclopropanecarboxylic acid of formula (2): 2with a monohydroxy compound of formula (3): R6OH??(3),in the presence of a catalyst compound comprising an element of to Group 4 of the Periodic Table of Elements.
Process for producing 2-fluorocyclopropancecarboxlic acid
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, (2008/06/13)
A process for producing a 2-fluorocyclopropane-carboxylic acid of formula ?I! STR1 by reducing a 2-halo-2-fluorocyclopropanecarboxylic acid of formula ?II! STR2 the reduction being carried out by developing a Raney nickel alloy in the presence of the 2-halo-2-fluorocyclo-propanecarboxylic acid of formula ?II!, or by contacting the 2-halo-2-fluorocyclopropanecarboxylic acid of formula ?II! with hydrogen in an aqueous solvent using a Raney nickel catalyst.
Selective dehalogenation process
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, (2008/06/13)
A compound represented by the following formula (1) or (3): STR1 is subjected to a catalytic hydrogenolysis reaction in the presence of a base and thus a compound represented by the following formula (2): STR2 wherein R represents a hydrogen atom or an al
Bicyclic amine derivatives
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, (2008/06/13)
A compound represented by formula (I) or a salt thereof: STR1 wherein X1 and X2 each represent a halogen atom; R1 represents a hydrogen atom or a substituent; R2 represents a substituted or unsubstituted bicyclic heterocyclic substituent of the following formula; STR2 wherein R3, R4, Y, Z, m, n, p, q and r are as defined herein; A represents a nitrogen atom or a substituted carbon atom; and R represents a hydrogen atom or a substituent. The compound exhibits potent antimicrobial activity and also high safety due to reduced lipophilicity.
Pyridonecarboxylic acid derivatives
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, (2008/06/13)
Quinolone derivatives are known as synthetic antimicrobial agents having a condensed pyridonecarboxylic acid skeleton, and those having substituents on various replaceable positions of said skeleton are known. In particular, if diastereomers exist, there are 4 or more kinds of stereoisomers. A mixture of diastereomers is a mixture of isomers having different physical properties and is difficult to apply as a drug as such. The present invention provides an antimicrobial 1-(1,2-cis-2-fluorocyclopropyl)-substituted quinolone derivative represented by formula I shown below which, although involving diastereomers, consists of a single stereoisomer. STR1 wherein R1 represents a methyl group, a difluoromethyl group, etc.; R2 represents a saturated nitrogen-containing heterocyclic group; A represents C--X3 or a nitrogen atom; X1 and X2 each represents a halogen atom; and X3 and Z represent a hydrogen atom, etc.
Optically active pyridonecarboxylic acid derivatives
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, (2008/06/13)
N1 -(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: STR1 These compounds have pate