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1. WO2019057951 - METHOD FOR PREPARATION OF DIFLUOROMETHYLORNITHINE

Publication Number WO/2019/057951
Publication Date 28.03.2019
International Application No. PCT/EP2018/075724
International Filing Date 24.09.2018
Chapter 2 Demand Filed 04.12.2018
IPC
C07C 229/26 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
26having more than one amino group bound to the carbon skeleton, e.g. lysine
CPC
C07C 227/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
227Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
14from compounds containing already amino and carboxyl groups or derivatives thereof
18by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
C07C 249/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
249Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton
02of compounds containing imino groups
C07C 251/24
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
251Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
02containing imino groups
24having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
Applicants
  • LONZA LTD [CH]/[CH]
Inventors
  • GUTMANN, Bernhard
  • BERSIER, Michael
  • HANSELMANN, Paul
  • KAPPE, Christian Oliver
  • KOECKINGER, Manuel
  • HONE, Christopher
Priority Data
17192830.225.09.2017EP
18151701.215.01.2018EP
18194996.718.09.2018EP
62/562,54625.09.2017US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) METHOD FOR PREPARATION OF DIFLUOROMETHYLORNITHINE
(FR) PROCÉDÉ DE PRÉPARATION DE DIFLUOROMÉTHYLORNITHINE
Abstract
(EN)
The invention discloses a method for preparation of protected difluoromethylornithine by a difluoromethylation of dibenzaldimine ornithine ester using CHF3 and LiHMDS (lithium bis(trimethylsilyl)amide), which can be converted to a salt of unprotected difluoromethylornithine by a subsequent deprotection under acidic conditions in the presence of water.
(FR)
L'invention concerne un procédé de préparation de difluorométhylornithine protégé par une difluorométhylation d'ester d'ornithine de dibenzaldimine à l'aide de CHF3 et de LiHMDS (bis(triméthylsilyl)amide de lithium), qui peut être converti en un sel de difluorométhylornithine non protégé par une déprotection ultérieure dans des conditions acides en présence d'eau.
Also published as
JP2020501496
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