WO2009004653A3 - Process for preparing an amorphous form of (2s,3s,5s)-2-(2,6- dimethylphenoxyacetyl)-amino-3-hydroxy-5-(2-(1-tetrahydropyrimid-2-only)-3-methylbutanoyl)-amino-1,6-diphenyl hexane and product thereof - Google Patents

Process for preparing an amorphous form of (2s,3s,5s)-2-(2,6- dimethylphenoxyacetyl)-amino-3-hydroxy-5-(2-(1-tetrahydropyrimid-2-only)-3-methylbutanoyl)-amino-1,6-diphenyl hexane and product thereof Download PDF

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Publication number
WO2009004653A3
WO2009004653A3 PCT/IN2008/000418 IN2008000418W WO2009004653A3 WO 2009004653 A3 WO2009004653 A3 WO 2009004653A3 IN 2008000418 W IN2008000418 W IN 2008000418W WO 2009004653 A3 WO2009004653 A3 WO 2009004653A3
Authority
WO
WIPO (PCT)
Prior art keywords
amino
lopinavir
amorphous form
tetrahydropyrimid
dimethylphenoxyacetyl
Prior art date
Application number
PCT/IN2008/000418
Other languages
French (fr)
Other versions
WO2009004653A2 (en
Inventor
Debashish Datta
Vellanki Siva Rama Prasad
Arabinda Sahu
Balusu Raja Babu
Putta Subba Rayudu
Ravi Mastan Rao
Umamaheswara Rao Vasireddy
Nagamahesh Yarlagadda
Om Dutt Tyagi
Original Assignee
Matrix Lab Ltd
Debashish Datta
Vellanki Siva Rama Prasad
Arabinda Sahu
Balusu Raja Babu
Putta Subba Rayudu
Ravi Mastan Rao
Umamaheswara Rao Vasireddy
Nagamahesh Yarlagadda
Om Dutt Tyagi
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 Matrix Lab Ltd, Debashish Datta, Vellanki Siva Rama Prasad, Arabinda Sahu, Balusu Raja Babu, Putta Subba Rayudu, Ravi Mastan Rao, Umamaheswara Rao Vasireddy, Nagamahesh Yarlagadda, Om Dutt Tyagi filed Critical Matrix Lab Ltd
Publication of WO2009004653A2 publication Critical patent/WO2009004653A2/en
Publication of WO2009004653A3 publication Critical patent/WO2009004653A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/10—Oxygen or sulfur atoms

Abstract

Disclosed herein is a process for preparing an amorphous form of (2S,3 S5SS)- 2-(2,6-dimethylphenoxyacetyl)-amiho-3-hydroxy-5-(2-(l-tetrahydropyrimid-2-only)- 3-methylbutanoyl)-amino-l,6-diphenyl hexane(Lopinavir), wherein lopinavir is dissolved in a solvent system, followed by removal of solvent employing drying technique and isolating the resultant pure amorphous form. Further process comprises of heating/drying the lopinavir at higher temperature to melt the solid and form uniform liquid, which is subjected to cooling arid drying to give amorphous lopinavir.
PCT/IN2008/000418 2007-07-04 2008-07-02 Process for preparing an amorphous form of (2s,3s,5s)-2-(2,6- dimethylphenoxyacetyl)-amino-3-hydroxy-5-(2-(1-tetrahydropyrimid-2-only)-3-methylbutanoyl)-amino-1,6-diphenyl hexane and product thereof WO2009004653A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN1438CH2007 2007-07-04
IN1438/CHE/2007 2007-07-04
IN409CH2008 2008-02-18
IN409/CHE/2008 2008-02-18

Publications (2)

Publication Number Publication Date
WO2009004653A2 WO2009004653A2 (en) 2009-01-08
WO2009004653A3 true WO2009004653A3 (en) 2009-02-26

Family

ID=40010634

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2008/000418 WO2009004653A2 (en) 2007-07-04 2008-07-02 Process for preparing an amorphous form of (2s,3s,5s)-2-(2,6- dimethylphenoxyacetyl)-amino-3-hydroxy-5-(2-(1-tetrahydropyrimid-2-only)-3-methylbutanoyl)-amino-1,6-diphenyl hexane and product thereof

Country Status (1)

Country Link
WO (1) WO2009004653A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2393786B1 (en) 2009-02-06 2014-01-22 Hetero Research Foundation Novel polymorphs of lopinavir
CA2837266A1 (en) 2011-05-27 2012-12-06 Hetero Research Foundation Amorphous ritonavir co-precipitated
CN106117148B (en) * 2016-06-17 2019-04-12 厦门市蔚嘉化学科技有限公司 A kind of preparation and purification technique of Lopinavir

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5914332A (en) * 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5914332A (en) * 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
STONER, ERIC J. ET AL: "Synthesis of HIV Protease Inhibitor ABT-378 (Lopinavir)", ORGANIC PROCESS RESEARCH & DEVELOPMENT , 4(4), 264-269 CODEN: OPRDFK; ISSN: 1083-6160, 2000, XP002505235 *

Also Published As

Publication number Publication date
WO2009004653A2 (en) 2009-01-08

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