32868-25-0Relevant articles and documents
Immunomodulator
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Paragraph 0294; 0299-0301, (2021/02/10)
The invention discloses an immunomodulator, and particularly relates to a compound shown as a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Experiments prove that the compound has good IL-17A inhibitory activity, can be used for preparing an IL-17A inhibitor and drugs for preventing and/or treating IL-17A mediated diseases (such as inflammation, autoimmune diseases, infectious diseases, cancers and precancerous syndromes), and provides a new medical possibility for clinical treatment of diseases related to abnormal IL-17A activity.
Preparation method of alminoprofen intermediate
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, (2021/07/21)
The invention discloses a preparation method of an alminoprofen intermediate, belongs to the field of organic chemical synthesis, and provides a new technical route for improving the defects of synthetic reaction of ethyl 2-(4-amino-phenyl)propionate: 1) taking p-fluoronitrobenzene and diethyl methylmalonate as raw materials, adding alkali, conducting heating, finishing the reaction, conducting cooling, conducting hydrolyzing with alkali, after the reaction is finished, conducting layering, conducting washing with water, extracting impurities, adjusting the pH value, extracting a product, and conducting concentrating to obtain AMLF02; 2) heating AMLF02 in a solvent to 55-75 DEG C, and dropwise adding thionyl chloride for esterification reaction, conducting cooling, adjusting the pH, directly adding a catalyst for reduction at the temperature of 70-80 DEG C, after the reaction is finished, conducting filtering with the aid of diatomite, neutralizing the filtrate to 7-8, conducting concentrating to remove ethanol, extracting a water phase with methylbenzene, and conducting concentrating to obtain AMLF04. The method has the beneficial effects that the problem of slow filtration is solved, extraction is omitted, time is saved, and cost is saved; direct layering is performed after reaction, the amount of hydrochloric acid is reduced, and the treatment difficulty of three wastes is reduced; and safe hydrazine hydrate replaces active nickel.
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors
Yoshikawa, Kenji,Yoshino, Toshiharu,Yokomizo, Yoshihiro,Uoto, Kouichi,Naito, Hiroyuki,Kawakami, Katsuhiro,Mochizuki, Akiyoshi,Nagata, Tsutomu,Suzuki, Makoto,Kanno, Hideyuki,Takemura, Makoto,Ohta, Toshiharu
scheme or table, p. 2133 - 2140 (2011/04/24)
We previously reported on a series of cyclohexanediamine derivatives as highly potent factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an alternative scaffold. Ethylenediamine derivatives possessing a substituent at the C1 position in S configuration and phenylenediamine derivatives possessing a substituent at the C5 position demonstrated moderate to strong anti-fXa activity. Further SAR studies led to the identification of compound 30h which showed both good in vitro activity (fXa IC50 = 2.2 nM, PTCT2 = 3.9 μM) and in vivo antithrombotic efficacy.
