CN106083891 Process For Preparing Compound Having Hiv Integrase Inhibitory Activity

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Office

China

Application Number 201610447148.9

Application Date 04.08.2011

Publication Number 106083891

Publication Date 09.11.2016

Grant Number 106083891

Grant Date 23.03.2018

Publication Kind B

IPC

CPC

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Applicants 盐野义制药株式会社

Inventors 隅野幸仁
冈本和也
柳井盛泰
山田大辅
五十岚史也

Agents 中国专利代理(香港)有限公司 72001
中国专利代理(香港)有限公司 72001

Priority Data 2010-175899 05.08.2010 JP
2010-277713 14.12.2010 JP

Title

(EN) Process For Preparing Compound Having Hiv Integrase Inhibitory Activity

(ZH) 具有HIV整合酶抑制活性的化合物的制造方法

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, or the like].

(ZH) 式（Y1）或式（Y2）（式中，RX为可被取代的碳环低级烷基等）所示的化合物或其盐的制造方法，其使用了式（X4）（式中，R1d为氢、卤素等，R2d为氢、可被取代基组E取代的低级烷基等，R4d为可被取代基组E取代的低级烷基等，以及R6d为可被取代基组E取代的低级烷基等）所示的吡啶酮衍生物的新的制造方法。

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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond 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 bond to halogen, e.g. ester or nitrile radicals
79	Acids; Esters

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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond 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 bond to halogen, e.g. ester or nitrile radicals
79	Acids; Esters

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

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1. CN106083891 - Process For Preparing Compound Having Hiv Integrase Inhibitory Activity

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

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