- Method for preparing potassium ion competitive retardant intermediate
-
The invention discloses a method for synthesizing a key intermediate compound 1 of a novel potassium ion competitive retardant fexuprazan, and belongs to the field of synthesis of medical intermediates. The invention aims to solve the problems of high preparation cost, low yield and the like of the compound 1, further improve the productivity and reduce the production cost. According to the method, 2, 4-difluorobenzylamine is used as a raw material, and a target product is obtained through condensation reaction, benzyl protection, cyclization under an alkaline condition, methylation, deprotection and the like in sequence. According to the method for synthesizing the compound 1, a novel process route is adopted, the yield is larger than 50%, and the method has the advantages of being novelin route, mild in reaction condition, low in cost and the like.
- -
-
-
- A 4 - methoxy pyrrole intermediate preparation method
-
The present invention provides 4 - methoxy pyrrole intermediate preparation method, comprises the following steps: (1) of formula (I) compound 2, 4 - difluorobenzaldehyde with formula (II) compound to the [...] sulfonic acid in the alkaline solvent and th
- -
-
Paragraph 0025; 0029-0030
(2019/07/10)
-
- METHOD FOR PREPARING INTERMEDIATE OF 4-METHOXYPYRROLE DERIVATIVE
-
The present invention relates to a.method for preparing intermediates of 4- methoxypyrrole derivatives. The preparation method according to the present invention has advantages that the production cost can be lowered by using inexpensive starting materials, a high-temperature reaction is not required as a whole, inexpensive and non-explosive reagents are used instead of (trimethylsilyl)diazomethane, and further an intermediate of 4-methoxypyrrole derivatives can be prepared as a whole at a high yield.
- -
-
-
- METHOD FOR PREPARING INTERMEDIATE OF 4-METHOXYPYRROLE DERIVATIVE
-
The present invention relates to a method for preparing intermediates of 4-methoxypyrrole derivatives. The preparation method according to the present invention has advantages that a high-temperature reaction is not required as a whole, inexpensive and non-explosive reagents are used instead of (trimethylsilyl)diazomethane, and further an intermediate of 4-methoxy pyrrole derivatives can be prepared as a whole at a high yield.
- -
-
-
- NOVEL ACID ADDITION SALT OF 1-(5-(2,4-DIFLUOROPHENYL)-1-((3-FLUOROPHENYL)SULFONYL)-4-METHOXY-1H-PYRROL-3-YL)-N-METHYLMETHANAMINE
-
The present invention provides a novel acid addition salt of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methoxy-1H-pyrrol-3-yl)-N-methylmethanamine. The acid addition salt has excellent proton pump inhibitory activity, gastric damaging activity and defense factor enhancing effect, and has excellent Helicobacter pylori (H. pylori) eradication activity to be usefully used in prevention and treatment of gastrointestinal tract, ulcers, gastritis, reflux esophagitis, or gastrointestinal damages by H. pylori.COPYRIGHT KIPO 2017
- -
-
Paragraph 0077; 0078
(2018/02/27)
-
- NOVEL CRYSTALLINE FORM OF 1-(5-(2,4-DIFLUOROPHENYL)-1-((3-FLUOROPHENYL)SULFONYL)-4-METHOXY-1H-PYRROL-3-YL)-N-METHYLMETHANAMINE SALT
-
Provided are a novel crystalline form I of 1-(5-(2,4-difluorophenyl)-1-((3-fluorophenyl)sulfonyl)-4-methyoxy-1H-pyrrol-3-yl)-N-methylmethanamin hydrochloride, a crystal form II of hydrochloride, a crystal form of succinate, a crystal form of tartrate, a crystal form I of fumarate and a crystal form II of fumarate. The novel crystal forms have high solubility with respect to water, have excellent stability under the damp proofing and high humidity exposure conditions and can be pharmaceutically used.COPYRIGHT KIPO 2017
- -
-
Paragraph 0164; 0174-0175
(2018/03/01)
-
- NOVEL 4-METHOXY PYRROLE DERIVATIVES OR SALTS THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
-
Provided are a 4-methoxy pyrrole derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The 4-methoxy pyrrole derivative or a pharmaceutically acceptable salt thereof has excellent proton pump inhibitory activity, inhibitory activity against gastric damage, and an effect of increasing defensive factors. In addition, the 4-methoxy pyrrole derivative or a pharmaceutically acceptable salt thereof has excellent bacteriostatic activity against Helicobacter pylori (H. pylori), and thus can be useful for preventing and treating gastrointestinal ulcer, gastritis, reflux esophagitis, or gastrointestinal damage caused by Helicobacter pylori (H. pylori). Moreover, the 4-methoxy pyrrole derivative or the pharmaceutically acceptable salt thereof has inhibitory activity against GPCR, and thus is useful for preventing and treating diseases mediated by a 5-HT receptor or a muscarinic acetylcholine receptor.COPYRIGHT KIPO 2016
- -
-
Paragraph 0218
(2016/10/10)
-