EP3127908 PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY

Office

European Patent Office

Application Number 16190894

Application Date 04.08.2011

Publication Number 3127908

Publication Date 08.02.2017

Publication Kind B1

IPC

CPC

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Applicants SHIONOGI & CO

Inventors SUMINO YUKIHITO
OKAMOTO KAZUYA
MASUI MORIYASU
YAMADA DAISUKE
IKARASHI FUMIYA

Designated States

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Priority Data 11814690 04.08.2011 EP
2010175899 05.08.2010 JP
2010277713 14.12.2010 JP

Title

(DE) VERFAHREN ZUR HERSTELLUNG EINER VERBINDUNG MIT HIV-INTEGRASE-HEMMENDER WIRKUNG

(EN) PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY

(FR) PROCÉDÉ POUR PRÉPARER UN COMPOSÉ AYANT UNE ACTIVITÉ INHIBITRICE D'INTÉGRASE DE VIH

Abstract

(EN) A process for preparing a compound represented by formula (Y1) or (Y2) [wherein R x is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R 1d is hydrogen, halogen, or the like; R 2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R 4d is a lower alkyl optionally substituted with substituent E, or the like; and R 6d is a lower alkyl group optionally substituted with substituent group E].

(FR) La présente invention concerne un procédé pour préparer un composé représenté par la formule (Y1) ou (Y2) [dans lesquelles R^x est un groupe carbocyclyl-(alkyle inférieur) facultativement substitué, ou similaire], utilisant un nouveau processus pour préparer un dérivé de pyridone représenté par la formule (X4) [dans laquelle R^1d est un hydrogène, un halogène, ou similaire; R^2d est un hydrogène, un groupe alkyle inférieur, ou similaire, ledit groupe alkyle inférieur étant facultativement substitué par un ou plusieurs choisis parmi le groupe de substituant E; R^4d est un groupe alkyle inférieur ou similaire, ledit groupe alkyle inférieur étant facultativement substitué par un ou plusieurs choisis parmi le groupe de substituant E; et R^6d est un groupe alkyle inférieur ou similaire, ledit groupe alkyle inférieur étant facultativement substitué par un ou plusieurs choisis parmi un groupe substituant E].

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
498	Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12	in which the condensed system contains three hetero rings
14	Ortho-condensed systems

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
498	Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12	in which the condensed system contains three hetero rings
14	Ortho-condensed systems

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
498	Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12	in which the condensed system contains three hetero rings
14	Ortho-condensed systems

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
213	Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02	having three double bonds between ring members or between ring members and non-ring members
04	having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60	with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78	Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79	Acids; Esters

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
B	GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200	Indexing scheme relating to specific properties of organic compounds
13	Crystalline forms, e.g. polymorphs

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1. EP3127908 - PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535	having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365	ortho- or peri-condensed with heterocyclic ring systems

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31	Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12	Antivirals
14	for RNA viruses
18	for HIV