HUP0003494A2 - Eljárás 2R-(1-hidroxi-1-trifluormetil-3-ciklopropilpropin-2-il)-4-klóranilin optikai tisztaságának fokozására - Google Patents

Eljárás 2R-(1-hidroxi-1-trifluormetil-3-ciklopropilpropin-2-il)-4-klóranilin optikai tisztaságának fokozására

Info

Publication number
HUP0003494A2
HUP0003494A2 HU0003494A HUP0003494A HUP0003494A2 HU P0003494 A2 HUP0003494 A2 HU P0003494A2 HU 0003494 A HU0003494 A HU 0003494A HU P0003494 A HUP0003494 A HU P0003494A HU P0003494 A2 HUP0003494 A2 HU P0003494A2
Authority
HU
Hungary
Prior art keywords
acid addition
addition salt
amino alcohol
suspension
optical purity
Prior art date
Application number
HU0003494A
Other languages
English (en)
Inventor
Cheng Yi Chen
Edward J. J. Grabowski
Paul J. Reider
Lushi Tan
Richard D. Tillyer
Original Assignee
Merck & Co., Inc.
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
Priority claimed from GBGB9721985.1A external-priority patent/GB9721985D0/en
Application filed by Merck & Co., Inc. filed Critical Merck & Co., Inc.
Publication of HUP0003494A2 publication Critical patent/HUP0003494A2/hu
Publication of HUP0003494A3 publication Critical patent/HUP0003494A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/82—Purification; Separation; Stabilisation; Use of additives
    • C07C209/86—Separation
    • C07C209/88—Separation of optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/10—Separation; Purification; Stabilisation; Use of additives
    • 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
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

A találmány tárgya eljárás a (3) képletű 2R-(1-hidroxi-1-trifluormetil-3-ciklopropilpropin-2-il)-4-klóranilin optikaitisztaságának fokozására. A találmány értelmében úgy járnak el, hogy(i) az aminoalkohol egy szerves oldószerrel készült oldatához lassansavas oldatot vagy gázt adnak az aminoalkohol savaddíciós sójáttartalmaz szuszpenzió képzése céljából; (ii) az aminoalkoholsavaddíciós sójának szuszpenzióját betöményítik; (iii) az aminoalkoholsavaddíciós sójának szerves oldószerrel alkotott, betöményítettszuszpenziójában az oldószer koncentrációját további oldószeradagolásával beállítják; (iv) az aminoalkohol savaddíciós sójáttartalmazó szuszpenziót a környezet hőmérsékletén mintegy 2 óra ésmintegy 24 óra közötti időn át állni hagyják; (v) az aminoalkoholsavaddíciós sójának így tárolt szuszpenzióját szűrik az aminoalkoholsavaddíciós sója által alkotott nedves szűrőlepény elkülönítésecéljából; (vi) az aminoalkohol savaddíciós sója alkotta nedvesszűrőlepényt hideg szerves oldószerrel mossák; és (vii) azaminoalkohol savaddíciós sója alkotta nedves szűrőlepényt szárítják azaminoalkohol savaddíciós sójának fokozott optikai tisztaságú szilárdanyagként való elkülönítése céljából. Ó
HU0003494A 1997-09-03 1998-09-01 Process for enhancing the optical purity of 2r-[1-hidroxy-1-trifluoromethyl-3-cyclo-propylpropyn-2yl]-4-chloroaniline HUP0003494A3 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US5789197P 1997-09-03 1997-09-03
GBGB9721985.1A GB9721985D0 (en) 1997-10-17 1997-10-17 Process for enhancing the optical purity
US9652998P 1998-08-13 1998-08-13
PCT/US1998/018104 WO1999011600A1 (en) 1997-09-03 1998-09-01 Process for enhancing the optical purity of 2r-[1-hydroxy- 1-trifluoromethyl- 3-cyclopropylpropyn-2yl] -4-chloroaniline

Publications (2)

Publication Number Publication Date
HUP0003494A2 true HUP0003494A2 (hu) 2001-10-28
HUP0003494A3 HUP0003494A3 (en) 2002-01-28

Family

ID=27269064

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0003494A HUP0003494A3 (en) 1997-09-03 1998-09-01 Process for enhancing the optical purity of 2r-[1-hidroxy-1-trifluoromethyl-3-cyclo-propylpropyn-2yl]-4-chloroaniline

Country Status (19)

Country Link
EP (1) EP1017666B1 (hu)
JP (1) JP4157272B2 (hu)
KR (1) KR20010023584A (hu)
CN (1) CN1276781A (hu)
AT (1) ATE253548T1 (hu)
AU (1) AU744536B2 (hu)
BR (1) BR9811437A (hu)
CA (1) CA2302011C (hu)
DE (1) DE69819538T2 (hu)
DK (1) DK1017666T3 (hu)
EA (1) EA002039B1 (hu)
ES (1) ES2209199T3 (hu)
HR (1) HRP20000120A2 (hu)
HU (1) HUP0003494A3 (hu)
NZ (1) NZ503121A (hu)
PL (1) PL338894A1 (hu)
PT (1) PT1017666E (hu)
SK (1) SK2932000A3 (hu)
WO (1) WO1999011600A1 (hu)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5952537A (en) * 1998-03-13 1999-09-14 Wiley Organics, Inc. Preparation of cycloalkylacetylene compounds using dialkylaminomagnesium halide or bis(dialkylamino)magnesium
GB0015981D0 (en) * 2000-06-29 2000-08-23 Glaxo Group Ltd Novel process for preparing crystalline particles
PE20060587A1 (es) * 2004-09-02 2006-07-09 Bristol Myers Squibb Co Sintesis de (s)-6-cloro-4-ciclopropiletinil-4-trifluorometil-1,4-dihidro-2h-3,1-benzoxazin-2-ona
CN102617367A (zh) * 2012-03-08 2012-08-01 浙江江北药业有限公司 (S)-5-氯-α-（环丙基乙炔）-2-氨基-α-（三氟甲基）苯甲醇晶型的制备
CN109761829A (zh) * 2019-02-19 2019-05-17 盐城迪赛诺制药有限公司 一种高手性纯度依非韦伦中间体的制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH498120A (de) * 1968-03-28 1970-10-31 Sandoz Ag Verfahren zur Herstellung neuer Indenopyridinderivate
US4085138A (en) * 1976-08-03 1978-04-18 Exxon Research & Engineering Co. Process for optical resolution of crude trans-1,2-cyclohexanediamine
DD285341B5 (de) * 1989-06-29 1993-08-26 Dresden Arzneimittel Verfahren zur herstellung der reinen enantiomeren des 1-(4-nitrophenoxy)-2-hydroxy-3-tert.-butylaminopropan und ihrer salze
IL106507A (en) * 1992-08-07 1997-11-20 Merck & Co Inc Pharmaceutical compositions containing benzoxazinones and some novel compounds of this type
US5442117A (en) * 1993-12-13 1995-08-15 Albemarle Corporation Enantiomeric resolution
JPH09208546A (ja) * 1995-11-29 1997-08-12 Ajinomoto Co Inc 新規置換ベンジルアミンの付加塩及びその光学分割法

Also Published As

Publication number Publication date
HRP20000120A2 (en) 2001-08-31
ATE253548T1 (de) 2003-11-15
JP2001514242A (ja) 2001-09-11
PT1017666E (pt) 2004-03-31
DE69819538D1 (de) 2003-12-11
DK1017666T3 (da) 2004-02-23
HUP0003494A3 (en) 2002-01-28
SK2932000A3 (en) 2001-01-18
AU744536B2 (en) 2002-02-28
CA2302011A1 (en) 1999-03-11
CA2302011C (en) 2008-05-13
PL338894A1 (en) 2000-11-20
EP1017666A1 (en) 2000-07-12
JP4157272B2 (ja) 2008-10-01
EA002039B1 (ru) 2001-12-24
WO1999011600A1 (en) 1999-03-11
KR20010023584A (ko) 2001-03-26
ES2209199T3 (es) 2004-06-16
EA200000279A1 (ru) 2000-08-28
NZ503121A (en) 2001-08-31
DE69819538T2 (de) 2004-09-30
EP1017666A4 (en) 2001-10-04
EP1017666B1 (en) 2003-11-05
CN1276781A (zh) 2000-12-13
AU9041898A (en) 1999-03-22
BR9811437A (pt) 2000-08-22

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