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1. CN103154004 - Process for preparing compound having HIV integrase inhibitory activity

Office
China
Application Number 201180048343.X
Application Date 04.08.2011
Publication Number 103154004
Publication Date 12.06.2013
Grant Number 103154004
Grant Date 06.07.2016
Publication Kind B
IPC
C07D 498/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
A61K 31/5365
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365ortho- or peri-condensed with heterocyclic ring systems
A61P 31/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
18for HIV
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
C07D 211/94
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
92with a hetero atom directly attached to the ring nitrogen atom
94Oxygen atom, e.g. piperidine N-oxide
CPC
C07D 498/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 213/79
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic 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
02having three double bonds between ring members or between ring members and non-ring members
04having 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
60with 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
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79Acids; Esters
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
A61K 31/5365
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5365ortho- or peri-condensed with heterocyclic ring systems
C07D 213/80
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic 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
02having three double bonds between ring members or between ring members and non-ring members
04having 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
60with 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
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
79Acids; Esters
80in position 3
C07D 211/94
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
92with a hetero atom directly attached to the ring nitrogen atom
94Oxygen atom, e.g. piperidine N-oxide
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 Rx is an optionally substituted carbocyclyl -lower-alkyl group, or the like], using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R1d is hydrogen, halogen, or the like; R2d is hydrogen, a lower alkyl group, or the like, said lower alkyl group being optionally substituted with one or more selected from substituent group E; R4d is a lower alkyl group or the like, said lower alkyl group being optionally substituted with one or more selected from substituent group E; and R6d is a lower alkyl group or the like, said lower alkyl group being optionally substituted with one or more selected from substituent group E].
(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,。