METHOD AND COMPOUND USEFUL IN PREPARING OREXIN-2 RECEPTOR ANTAGONIST, AND LEMBOREXANT CONTAINING SMALL AMOUNT OF IMPURITIES Russian patent published in 2024 - IPC C07C67/14 C07C69/67 C07D401/12 C07D239/34 C07C303/28 C07C309/73 

Abstract RU 2823998 C2

FIELD: chemistry.

SUBSTANCE: present invention relates to a method of producing a compound of formula III. Proposed method includes: a) adding a Grignard reagent to a mixture containing a compound of formula II, toluene and tetrahydrofuran at 60 °C or lower; and b) adding the obtained mixture to a mixture containing acetyl chloride and ethyl acetate at 20 °C or lower. Also disclosed are methods of producing compounds of formula XI, formula IX, formula VII, formula V and formula IV.

EFFECT: invention enables to provide a method for synthesis of a compound of formula III, which is suitable for preparing a compound of formula XI (lemborexant) containing a small amount of impurities.

10 cl, 3 ex, 2 tbl

, , , , ,

Similar patents RU2823998C2

Title Year Author Number
METHODS AND COMPOUNDS THAT CAN BE USED TO SYNTHESIZE OREXIN-2 RECEPTORS ANTAGONISTS 2013
  • Moniz Dzhordzh Entoni
  • Uilkoksen Enni Zhu
  • Benajud Farid
  • Li Dzaemoon
  • Chzhan Khojmin
  • Terauti Taro
  • Takemura Ayumi
  • Josida Yu
  • Tanaka Tosiaki
  • Sorimati Keiiti
  • Naoe Josimitsu
  • Kadzuta Yudzi
RU2617696C2
CYCLOPROPANE COMPOUNDS 2011
  • Terauti Taro
  • Takemura Ajumi
  • Doko Takasi
  • Josida Ju
  • Tanaka Tosiaki
  • Sorimati Keiiti
  • Naoe Esimitsu
  • Bojkmann Karsten
  • Kazuta Judzi
RU2571414C2
CONDENSED AMINODIHYDROTHIAZINE DERIVATIVES APPLICABLE AS BACE INHIBITORS 2012
  • Kholl Adrian
  • Farting Kristofer Nil
  • Kastro Pinejro Khose Luis
RU2593756C2
COMPOSITIONS AND METHODS OF TREATING ANDROGEN-RECEPTOR-POSITIVE CANCER 2020
  • Caligiuri, Maureen
  • Ericsson, Anna
  • Guichard, Sylvie
  • Xu, Qunli
RU2817802C2
METHOD FOR PRODUCING PYRIMIDIN-1-OL COMPOUND AND ITS INTERMEDIATE COMPOUND 2015
  • Watanabe Yuzo
RU2681937C2
SUBSTITUTED HETEROCYCLIC SULPHONAMIDE COMPOUNDS USEFUL AS TRPA1 MODULATORS 2014
  • Chen Khuejfen
  • Chu Yanyan
  • Do Stiven
  • Estrada Entoni
  • Khu Bajkhua
  • Kolesnikov Aleksandr
  • Lin Sinyuj
  • Lissikatos Dzhozef P.
  • Shor Daniel
  • Verma Vishal
  • Vang Lan
  • U Goshen
  • Yuen Po-Vaj
RU2675792C2
METHODS OF PREPARING 1,3-BENZODIOXOL HETEROCYCLIC COMPOUNDS 2018
  • Dal, Allan Karsten
  • Bajtner, Jokhan Eriksson
  • Olsen, Esben Paul Krogkh
  • Metsler, Bern
RU2814175C2
DERIVATIVE OF DI- AND TRIAZOLYLPROPANE, METHODS OF ITS SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF 1996
  • Katsumi Itokh
  • Kendzi Okonogi
  • Akikhiro Tasaka
RU2145605C1
METHODS AND INTERMEDIATE COMPOUNDS FOR OBTAINING MACROCYCLIC INHIBITORS OF PROTEASE HCV 2011
  • Ormirod Dominik Dzhon
  • Depre Dominik Pol Mishel
  • Khorvat Andrash
RU2628081C2
DERIVATIVES OF AZOLE, METHODS OF THEIR SYNTHESIS AND ANTIFUNGAL AGENT 1994
  • Katsumi Iton
  • Kendzi Okonogi
  • Akikhiro Tasaka
RU2131417C1

RU 2 823 998 C2

Authors

Abe Taichi

Yoshizawa Kazuhiro

Watanabe Yuzo

Miura Takeshi

Ayata Yusuke

Yasuda Yoshinori

Dates

2024-07-31Published

2020-05-13Filed