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1. WO2016065290 - SEMI-SYNTHESIS PROCEDURES

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Publication Number WO/2016/065290
Publication Date 28.04.2016
International Application No. PCT/US2015/057167
International Filing Date 23.10.2015
IPC
C07D 207/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04having no double bonds between ring members or between ring members and non-ring members
06with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07C 231/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
12by reactions not involving the formation of carboxamide groups
C07C 245/20 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
245Compounds containing chains of at least two nitrogen atoms with at least one nitrogen-to-nitrogen multiple bond
20Diazonium compounds
C07C 237/26 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
24having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
26of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
CPC
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
C07C 231/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
12by reactions not involving the formation of carboxamide groups
C07C 237/26
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
24having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
26of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
C07C 245/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
245Compounds containing chains of at least two nitrogen atoms with at least one nitrogen-to-nitrogen multiple bond
20Diazonium compounds
C07C 2603/46
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2603Systems containing at least three condensed rings
02Ortho- or ortho- and peri-condensed systems
40containing four condensed rings
42containing only six-membered rings
44Naphthacenes; Hydrogenated naphthacenes
461,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines
C07D 207/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04having no double bonds between ring members or between ring members and non-ring members
06with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
Applicants
  • TETRAPHASE PHARMACEUTICALS, INC. [US]/[US]
Inventors
  • ZHANG, Wu-Yan
  • LAFRANCE, Danny
  • RONN, Magnus, P.
Agents
  • ABELLEIRA, Susan, M.
Priority Data
62/067,69723.10.2014US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) SEMI-SYNTHESIS PROCEDURES
(FR) PROCÉDURES DE SEMI-SYNTHÈSE
Abstract
(EN) Provided herein are improved processes tor convening C7-amino-substituted tetracyclines to C7-fluoro-substituted tetracyclines, as well as intermediates produced by or used in these processes. In one embodiment, a thermal fluorination method is provided in which a suspension comprising a non-polar organic solvent and a C7-diazo-substituted tetracycline hexafluorophosphate, hexafluoarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof, is healed to provide a C7-fluoro-substituted tetracycline, or salt, solvate or combination thereof. In another embodiment, a photolytic fluorination is provided in which a solution comprising an ionic liquid and a C-7diazo-substituted tetracycline tetrafluoroborate, hexafluorophosphate, hexafluoroarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof, is irradiated to provide a C7-fluoro-substituted tetracycline, or salt, solvate or combination thereof.
(FR) La présente invention concerne des procédés améliorés pour transformer des tétracyclines à substitution C7-amino en tétracyclines à substitution C7-fluoro, ainsi que des intermédiaires produits ou utilisés dans ces procédés. Dans un mode de réalisation, un procédé de fluoration thermique est prévu selon lequel une suspension comprenant un solvant organique non polaire et une tétracycline à substitution C7-diazo-hexafluorophosphate, un hexafluoarsenate ou un sel d'hexafluorosilicate, ou un sel, un solvate ou une combinaison de ceux-ci, est réparée pour fournir une tétracycline à substitution C7-fluoro, ou un sel, un solvate ou une combinaison de ceux-ci. Dans un autre mode de réalisation, une fluoration photolytique est prévue selon laquelle une solution comprenant un liquide ionique et un sel tétrafluoroborate, hexafluorophosphate, hexafluoroarséniate ou hexafluorosilicate de tétracycline à substitution C-7 diazo, ou un sel, un solvate ou une combinaison de ceux-ci, est irradiée pour fournir une tétracycline à substitution C7-fluoro, ou un sel, un solvate ou une combinaison de ceux-ci.
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