cas 80382-23-6, Loxoprofen sodium | Articles data

Articles about 80382-23-6Total 10 be found

Synthesis method of loxoprofen sodium
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.
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Paragraph 0048; 0050; 0056; 0061-0062

(2019/06/07)

New method for synthesizing loxoprofen sodium
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.
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Paragraph 0008; 0011

(2019/06/08)

Loxoprofen sodium dihydrate crystal form and preparation method thereof
The invention relates to a loxoprofen sodium dihydrate crystal form preparation method thereof. The loxoprofen is dissolved in a dissolving solvent and reacted with sodium-containing base to prepare loxoprofen sodium, and after adding water, the seed crystal may or may not be added to prepare the loxoprofen sodium dihydrate crystal form. The crystal form preparation method obtains the high-puritycrystal form, and the novel crystal form has good fluidity and appearance.
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Paragraph 0034-0041

(2019/01/10)

Loxoprofen sodium preparation method
The invention discloses a loxoprofen sodium preparation method, which comprises: directly carrying out alkylation on 2-(p-bromomethyl)isophenylpropionic acid as a starting raw material under a NaOH and DMF system, carrying out hydrolysis decarboxylating to obtain a crude product, separating the by-product produced in the reaction through high-vacuum distillation to obtain loxoprofen acid, and carrying out salt forming to obtain the loxoprofen sodium. According to the present invention, the method has characteristics of less synthesis step, mild reaction condition, reasonable price and easy purchase of the raw material, low pollution and low production cost, and is suitable for industrial production, wherein the product content can reach more than 99.8%, and the single impurity is less than0.05%.
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Paragraph 0022-0029

(2019/05/11)

Loxoprofen derivative
The invention provides a Loxoprofen derivative shown in the following formula (I). R1 is hydrogen atoms or substituted or non-substituted alkyl, R2 is substituted or non-substituted alkyl, the Loxoprofen derivative has low gastrointestinal tract side effects, and the bioavailability can be improved. The formula (I) is shown in the specification.
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Paragraph 0036; 0037; 0039; 0044

(2019/01/23)

Method for synthesizing high-purity non-steroidal anti-inflammatory drug loxoprofen sodium
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%.
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Paragraph 0076; 0077; 0078; 0079; 0080

(2018/09/13)

Loxoprofen sodium and preparation method of intermediate of loxoprofen sodium
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.
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Paragraph 0067; 0068; 0069

(2017/09/29)

Method for preparing loxoprofen sodium
The invention relates to the technical field of organic synthesis, in particular to a method for preparing loxoprofen sodium. The invention provides a compound with the structure shown in formula 5 and a preparation method and application of the compound, (the formula is defined in the description). The loxoprofen sodium obtained according to the scheme is high in purity, high in industrialized operation, and good in application prospect.
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Paragraph 0116-0118

(2017/07/12)

Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl) methyl]phenyl}propanoic acid: Nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities
We previously proposed that membrane permeabilization activity of NSAIDs is involved in NSAID-induced gastric lesions. We here synthesized derivatives of loxoprofen that have lower membrane permeabilization activity than other NSAIDs. Compared to loxoprofen, the derivatives 10a and 10b have lower membrane permeabilization activity and their oral administration produced fewer gastric lesions but showed an equivalent anti-inflammatory effect. These results suggest that 10a and 10b are likely to be therapeutically beneficial as safer NSAIDs.
Yamakawa, Naoki,Suemasu, Shintaro,Matoyama, Masaaki,Kimoto, Ayumi,Takeda, Miho,Tanaka, Ken-Ichiro,Ishihara, Tomoaki,Katsu, Takashi,Okamoto, Yoshinari,Otsuka, Masami,Mizushima, Tohru
supporting information; experimental part
p. 7879 - 7882
(2011/02/22)

Ophthalmic anti-inflammatory agents
Compounds of formula: STR1 (wherein R represents hydrogen or methyl, >A--B-- represents a >CH--CH2 -- or >C=CH-- group; >C--Z represents a >C=O or >CH--OH group; and n represents 1 or 2) and ophthalmically acceptable salts and esters thereof are useful as ophthalmic anti-inflammatory agents.
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(2008/06/13)