WO2016159666A3 - Crystal form and preparation method therefor - Google Patents

Crystal form and preparation method therefor Download PDF

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Publication number
WO2016159666A3
WO2016159666A3 PCT/KR2016/003285 KR2016003285W WO2016159666A3 WO 2016159666 A3 WO2016159666 A3 WO 2016159666A3 KR 2016003285 W KR2016003285 W KR 2016003285W WO 2016159666 A3 WO2016159666 A3 WO 2016159666A3
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
crystal form
method therefor
present
hygroscopicity
Prior art date
Application number
PCT/KR2016/003285
Other languages
French (fr)
Korean (ko)
Other versions
WO2016159666A2 (en
Inventor
박상욱
임종재
김철우
송세현
손세일
이홍우
Original Assignee
대원제약주식회사
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 대원제약주식회사 filed Critical 대원제약주식회사
Priority to CN201680020018.5A priority Critical patent/CN107438595B/en
Publication of WO2016159666A2 publication Critical patent/WO2016159666A2/en
Publication of WO2016159666A3 publication Critical patent/WO2016159666A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/335—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • C07D309/10—Oxygen atoms
    • C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

A preparation method of the present invention can produce 4-(((tetrahydro-pyran-2-yl)oxy)methyl) aniline with high yield and purity in spite of low costs. In addition, a crystal form of the present invention is remarkably excellent in stability, hygroscopicity, and solubility.
PCT/KR2016/003285 2015-03-31 2016-03-30 Crystal form and preparation method therefor WO2016159666A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201680020018.5A CN107438595B (en) 2015-03-31 2016-03-30 Crystal form and preparation method thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2015-0045649 2015-03-31
KR1020150045649A KR102013157B1 (en) 2015-03-31 2015-03-31 Crystalline form and Method of preparing the same

Publications (2)

Publication Number Publication Date
WO2016159666A2 WO2016159666A2 (en) 2016-10-06
WO2016159666A3 true WO2016159666A3 (en) 2017-01-26

Family

ID=57004474

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2016/003285 WO2016159666A2 (en) 2015-03-31 2016-03-30 Crystal form and preparation method therefor

Country Status (3)

Country Link
KR (1) KR102013157B1 (en)
CN (1) CN107438595B (en)
WO (1) WO2016159666A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102001835B1 (en) * 2018-08-24 2019-07-19 대원제약주식회사 Method of preparing (3r,5r)-7-(2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-((4-hydroxymethylphenylamino)carbonyl)-pyrrol-1-yl)-3,5-dihydroxy-heptanoic acid hemi calcium salt, intermediates used therein, and method of preparing the intermediates
KR102218320B1 (en) * 2019-07-12 2021-02-23 대원제약주식회사 Method of preparing(3r,5r)-7-(2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-((4-hydroxymethylphenylamino)carbonyl)-pyrrol-1-yl)-3,5-dihydroxy-heptanoic acid hemi calcium salt, and method of preparing intermediates used therein

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060084816A1 (en) * 2001-08-16 2006-04-20 Biocon Limited Process for the production of atorvastatin calcium
US20080153896A1 (en) * 2006-07-14 2008-06-26 Gyan Chand Yadav Polymorphic Forms of an HMG-CoA Reductase Inhibitor and Uses Thereof
US20100056602A1 (en) * 2003-05-30 2010-03-04 Ranbaxy Laboratories Limited Substituted Pyrrole Derivatives And Their Use As HMG-CO Inhibitors
WO2011153247A1 (en) * 2010-06-01 2011-12-08 Furiex Pharmaceuticals, Inc. Combination therapies
KR101329113B1 (en) * 2005-11-08 2013-11-14 랜박시 래보러터리스 리미티드 Process for preparation of (3r,5r)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxy methyl phenyl amino)carbonyl]-pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid hemi calcium salt

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002155033A (en) * 2000-11-22 2002-05-28 Nippon Kayaku Co Ltd Method for producing aminobenzylalcohol compounds
CN101304968A (en) * 2005-11-08 2008-11-12 兰贝克赛实验室有限公司 Process for (3r, 5r)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4- [(4-hydroxy methyl phenyl amino) carbonyl]-pyrrol-1-yl]-3, 5-dihydroxy-heptanoic acid hemi calcium salt

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060084816A1 (en) * 2001-08-16 2006-04-20 Biocon Limited Process for the production of atorvastatin calcium
US20100056602A1 (en) * 2003-05-30 2010-03-04 Ranbaxy Laboratories Limited Substituted Pyrrole Derivatives And Their Use As HMG-CO Inhibitors
KR101329113B1 (en) * 2005-11-08 2013-11-14 랜박시 래보러터리스 리미티드 Process for preparation of (3r,5r)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxy methyl phenyl amino)carbonyl]-pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid hemi calcium salt
US20080153896A1 (en) * 2006-07-14 2008-06-26 Gyan Chand Yadav Polymorphic Forms of an HMG-CoA Reductase Inhibitor and Uses Thereof
WO2011153247A1 (en) * 2010-06-01 2011-12-08 Furiex Pharmaceuticals, Inc. Combination therapies

Also Published As

Publication number Publication date
KR102013157B1 (en) 2019-08-23
KR20160117843A (en) 2016-10-11
WO2016159666A2 (en) 2016-10-06
CN107438595B (en) 2021-05-18
CN107438595A (en) 2017-12-05

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