68767-14-6Relevant articles and documents
Preparation method of loxoprofen
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, (2020/07/27)
The invention discloses a novel preparation method of loxoprofen (I). The reaction process comprises the following steps: a compound (VII) and a compound (VIII) are subjected to a condensation reaction to obtain an intermediate (IX), the intermediate (IX) is subjected to a hydrogenation reduction reaction in a mixed solvent of acid and alcohol to obtain an intermediate (X), and the intermediate (X) is subjected to a hydrolysis reaction to obtain loxoprofen (I).
Preparation method of aryl propionic acid compound
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Page/Page column 0121-0125, (2020/10/04)
The invention provides a preparation method of an aryl propionic acid compound, wherein the preparation method comprises the following steps: carrying out acetylation reaction on substituted aryl benzene to obtain aryl acetophenone; carrying out hydrogenation reduction reaction on alpha-substituted aryl ethyl ketone to obtain alpha-substituted aryl ethanol; and in an acidic solution, introducing carbon monoxide gas into the alpha-substituted aryl ethanol, and carrying out a carbonylation reaction under the co-catalytic action of a main catalyst and a cocatalyst to obtain the aryl propionic acid compound, wherein the cocatalyst has the following structural formula described in the specification, R1 is one of hydrogen and a substituted carboxylic acid group, and R2 is one of hydrogen, halogen, substituted or unsubstituted C1-C12 alkyl, substituted or unsubstituted C1-C6 alkoxy, substituted or unsubstituted C3-C12 naphthenic base, substituted carbonyl containing C6-C24 aryl or substitutedaryl, substituted carbonyl containing C3-C12 heterocyclic radical or substituted heterocyclic radical, phenyl, substituted phenyl, naphthyl and substituted naphthyl.
Synthetic method of loxoprofen
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Paragraph 0034; 0083; 0089-0090; 0095; 0100-0101, (2020/08/02)
The invention discloses a synthetic method of an intermediate loxoprofen for preparing a phenylpropionic acid non-steroidal anti-inflammatory drug loxoprofen sodium. The synthetic method comprises thefollowing steps: firstly, carrying out acylation reaction on a compound VII and a compound VIII in a solvent 1 under the action of lewis acid serving as a catalyst to obtain an intermediate compoundIX; and introducing hydrogen into the intermediate compound IX in a solvent 2 under the action of strong acid by taking palladium on carbon as a catalyst, and carrying out hydrogenation tert-butyl ester removal reaction to obtain loxoprofen. The synthetic method has the advantages that the synthetic route is short, simple in process and convenient to operate, no corrosive strong acid is used in the synthesis process, and the reaction control temperature in the synthesis process is relatively mild; and the synthetic method has the characteristics of no product carbonization, no corrosion to equipment, safe and environment-friendly synthesis process, suitability for industrial production and the like, and the finally obtained product loxoprofen has high yield which can reach 65.8-73.3% and purity of 99.54-99.69% from the beginning of the compound VIII.
Preparation method for substituted phenylacetic acid derivative
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, (2019/03/29)
The invention belongs to the field of medicament synthesis, relates to a preparation method for a substituted phenylacetic acid derivative, in particular to a preparation method for preparing 2-[4-(2-oxygen amyl methyl)phenylpropionic acid]. A dihalobenzyl compound or a disubstituted benzyl compound reacts with a compound of cyclopentanone or a precursor form compound thereof to prepare a precursor compound of Loxoprofen which is as shown in the description, wherein X is a halogen, L1 is a halogen, OH, OMs, OTs and OTf, L2 is a halogen, a cyanogroup, a hydroxide radical, -CH2OH, -CHO, nitromethane, an ester group, -NR4R5, OTf, OTs, OMs, -C=CR6 and -C is equivalent to CR7, wherein R4, R5, R6 and R7 are low substituted alkyl group; Z is cyclopentanone or the precursor form thereof; the precursor form is as shown in the description; and R3 is a low substituted alkyl group. Further, the preparation method comprises a step of converting the cyclopentanone precursor form into cyclopentanone;and the precursor compound of the Loxoprofen is used for preparing a Loxoprofen compound.
A substituted phenylacetic acid derivatives (by machine translation)
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, (2019/04/18)
The invention belongs to the field of drug synthesis, relates to a substituted phenylacetic acid derivatives, in particular to the preparation of 2 - [4 - (2 - methyl oxygen fifth heavenly stem) hydrocinnamic acid] preparation method. If nitrile alkylation reaction include alkylation reaction, reaction or ester alkyl [...] reaction to prepare the intermediate type II - 2 or type II - 2' compound, After the hydrolytic reaction or oxidation reaction preparation to obtain the product. The invention relates to the alkylation reaction without additional solvent, is a more industrialization of the advantages of the line. (by machine translation)
New method for synthesizing loxoprofen sodium
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Paragraph 0008; 0010, (2019/06/08)
The invention belongs to the field of synthesis of organic matters and specifically relates to a new method for synthesizing loxoprofen sodium. The synthesis method is characterized by taking 2-(4-bromomethyl) phenylpropionic acid as a raw material and performing a 4-step reaction to prepare the loxoprofen sodium. The new method for synthesizing the loxoprofen sodium adopted by the invention has the effects that the yield is increased and the industrial prospect is good.
Synthesis method of loxoprofen sodium
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, (2019/06/07)
The invention discloses a synthesis method of loxoprofen sodium, which comprises the following steps of: step 1), preparing N-(1-cyclopentenyl) morpholine; step 2), preparing 2-(4-bromomethyl phenyl)methyl propionate, the method also comprises the following step 3), preparing loxoprofen sodium by an enamine alkylation method: first dissolving 2-(4-bromomethyl phenyl) methyl propionate in a solvent, adding N-(1-cyclopentenyl) morpholine and the solvent in a container, dropwise adding 2-(4-bromomethyl phenyl) methyl propionate solution under reflux conditions; continuing reacting under reflux conditions after the completion of the dropwise addition; adding alkali solution after obtained reaction liquid is cooled, hydrolysising and separating to obtain an organic phase and an aqueous phase respectively, extracting the aqueous phase with an extractant to obtain extract liquid and the aqueous phase after extraction respectively, and post-treating the aqueous phase after extraction to obtain loxoprofen sodium. The preparation of loxoprofen sodium by the above method has the advantages of simple reaction steps, high yield of loxoprofen sodium and low production cost.
Method for synthesizing high-purity non-steroidal anti-inflammatory drug loxoprofen sodium
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Paragraph 0064; 0065; 0066; 0067; 0068, (2018/09/13)
The invention discloses a method for synthesizing high-purity non-steroidal anti-inflammatory drug loxoprofen sodium, 2-(4-bromomethylphenyl) methyl propionate b is synthesized by esterification of raw material a and methanol, intermediate compound c and loxoprofen acid are synthesize sequentially, and the loxoprofen sodium is finally synthesized. The reaction mechanism is simple, by-products arefew, synthesis steps are easy to control, the raw material is easily available, and the impurity content of each step is strictly controlled. The purifying method is easy to operate and suitable for industrial production. The white flake crystal loxoprofen sodium is prepared. Finally, HPLC analysis shows that the loxoprofen sodium content detected by HPLC is as high as 99.95%.
Loxoprofen sodium and preparation method of intermediate of loxoprofen sodium
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, (2017/09/29)
The invention relates to the technical field of organic synthesis and in particular relates to loxoprofen sodium and a preparation method of an intermediate of the loxoprofen sodium. The invention provides a compound with a structure shown as a formula A: the formula A is shown in the description, wherein R and R are independently selected from methyl or ethyl or can be subjected to cyclic synthesis to form a formula shown in the description respectively, wherein n is 1 or 2; Y is X or a formula shown in the description, wherein X is Cl or Br and R is methyl or ethyl.
GLYCOSAMINOGLYCAN DERIVATIVE AND METHOD FOR PRODUCING SAME
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Paragraph 0416-0420, (2016/06/28)
The present invention provides a glycosaminoglycan derivative in which a group derived from glycosaminoglycan and a group derived from a physiologically active substance having at least one of a carboxy group and a hydroxy group are coupled by covalent bond with a spacer therebetween, in which the spacer is selected in accordance with the decomposition rate of the covalent bond to the group derived from the physiologically active substance.
