METHODS AND INTERMEDIATE PRODUCTS Russian patent published in 2011 - IPC C07D405/12 C07B43/04 C07B61/00 B01J31/24 A61P43/00 C07B57/00 B01J23/44 B01J31/16 A61K31/4025 

Abstract RU 2433127 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I , isomer thereof of formula IA , mixture of isomers thereof IA/C , synthesis method thereof, as well as methods of producing compounds of formula IVA from compounds of formula IA, involving reduction and removal of protection from compounds of formula IA via hydrogenolysis using H2 and a catalytic amount of Pd/C, in the presence of trifluoroacetic acid to obtain a compound of formula VA; further reaction of this compound with Cbz-t-leu-OH, EDC and HOBt to obtain a compound of formula VIA; reaction of compound VIA with H2 and a catalytic amount of Pd/C in the presence of citric acid to obtain an amine and reaction of said amine and 4-amino-3-chlorobenzoic acid in the presence of CDMT and NMM to obtain a compound of formula IVA.

EFFECT: fewer synthesis steps and high output while using dynamic crystallisation.

13 cl, 5 ex

Similar patents RU2433127C2

Title Year Author Number
METHODS AND INTERMEDIATE COMPOUNDS 2010
  • Tehnouri Dzheral'D Dzh.
  • Chehn' Min'Chzhan
  • Koshrehn Dzhon Eh.
  • Luker Adam
  • Jurkauskas Valdas
RU2531588C2
METHODS AND INTERMEDIATE PRODUCTS 2006
  • Tehnouri Dzheral'D Dzh.
  • Chen' Min'Chzhan
  • Koshrehn Dzhon Eh.
RU2446171C2
MACROCYCLISATION REACTION AND INTERMEDIATE COMPOUND AND OTHER FRAGMENTS, USEFUL IN SYNTHESIS OF MACROLIDES OF HALICHONDRINS 2016
  • Fang, Francis, G.
  • Chase, Charles, E.
  • Kim, Dae-Shik
  • Choi, Hyeong-Wook
RU2739034C2
METHODS AND INTERMEDIATE COMPOUNDS FOR PRODUCING STERIC COMPOUNDS 2007
  • Tehnouri Dzheral'D Dzh.
  • Chen' Min'Chzhan
  • Dzung Joung Chun'
  • Forslund Rehjmond E.
RU2481326C2
MACROCYCLIZATION REACTIONS AND INTERMEDIATE COMPOUNDS AND OTHER FRAGMENTS SUITABLE FOR PREPARING ANALOGUES OF HALICHONDRIN B 2014
  • Fan Frensis Dzh.
  • Kim Dae-Sik
  • Choj Khieong-Vook
  • Chejz Charlz I.
  • Li Dzaemoon
RU2710545C2
PRINCE REACTION AND COMPOUNDS USED IN SYNTHESIS OF HALICHONDRIN MACROLIDES AND THEIR ANALOGUES 2019
  • Choi, Hyeong-Wook
  • Fang, Francis G.
RU2813146C2
PRINCE REACTION AND INTERMEDIATE PRODUCTS USED IN SYNTHESIS OF HALICHONDRIN MACROLIDES AND THEIR ANALOGUES 2017
  • Chase, Charles, E.
  • Choi, Hyeong-Wook
  • Endo, Atsushi
  • Fang, Francis, G.
  • Kim, Dae-Shik
RU2777913C2
METHOD OF PRODUCING 2,3-DISUBSTITUTED INDOLES 2006
  • Kkhodabokus Akhmad
  • Lju Chzhisjuj
  • Senanajake Kris Kh'Ju
  • Vehj Khan'Sjun'
  • Chzhan Jonda
RU2466126C2
MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 2006
  • De Kok Kherman Augustinus
  • Rabuasson P'Er Zhan-Mari Bernar
  • Takhri Abdellakh
  • Simmen Kennet Alan
  • Nil'Sson Karl Magnus
  • Samuehl'Sson Bengt Bertil
  • Rosenkvist Osa Annika Kristina
  • Antonov Dmitrij
RU2441870C2
HEPATITIS C VIRUS MACROCYCLIC INHIBITORS 2006
  • Rabuasson P'Er Zhan-Mari Bernar
  • De Kok Kherman Augustinus
  • Khu Lili
  • Sjurlero Dominik Lui Nestor Gilehjn
  • Simmen Kennet Alan
  • Sal'Vador Oden Lourdes
  • Nil'Sson Karl Magnus
  • Rosenkvist Osa Annika Kristina
  • Samuehl'Sson Bengt Bertil
RU2486189C2

RU 2 433 127 C2

Authors

Tehnauri Dzheral'D Dzh.

Chen' Min'Chzhan

Dzhouns Ehndrju D.

Najs Filip L.

Trjudo Martehn

Gerin Dehvid Dzh.

Snunian Dzhon R.

Dates

2011-11-10Published

2005-03-11Filed