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AR101319A1 - QUIRAL RESOLUTION OF THE ESTERS OF THE ACID 4-ARIL-2-TIAZOL-2-IL-1,4-DIHYDROPIRIMIDIN-5-CARBOXYL - Google Patents

QUIRAL RESOLUTION OF THE ESTERS OF THE ACID 4-ARIL-2-TIAZOL-2-IL-1,4-DIHYDROPIRIMIDIN-5-CARBOXYL

Info

Publication number
AR101319A1
AR101319A1 ARP150102373A ARP150102373A AR101319A1 AR 101319 A1 AR101319 A1 AR 101319A1 AR P150102373 A ARP150102373 A AR P150102373A AR P150102373 A ARP150102373 A AR P150102373A AR 101319 A1 AR101319 A1 AR 101319A1
Authority
AR
Argentina
Prior art keywords
formula
dihydropirimidin
quiral
tiazol
aril
Prior art date
Application number
ARP150102373A
Other languages
Spanish (es)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR101319A1 publication Critical patent/AR101319A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B57/00—Separation of optically-active compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Procedimiento para la preparación de un éster del ácido 4-fenil-6-metil-2-tiazol-2-il-1,4-dihidropirimidín-5-carboxílico enantioméricamente puro, el compuesto de fórmula (1a), en el que R¹ es fenilo, que se encuentra no sustituido, o una, dos o más veces sustituido con halógeno, R² es alquilo C₁₋₆, caracterizado porque el procedimiento comprende las etapas siguientes: Etapa a) formación y recristalización de la sal enantiomérica de fórmula (2), o solvato; Etapa b) recuperación del compuesto enantiomérico de fórmula (1) a partir de su sal enantiomérica de fórmula (2) o solvato.Claim 1: Process for the preparation of an enantiomerically pure 4-phenyl-6-methyl-2-thiazol-2-yl-1,4-dihydropyrimidine-5-carboxylic acid ester, the compound of formula (1a), in the that R¹ is phenyl, which is unsubstituted, or one, two or more times substituted with halogen, R² is C₁₋₆ alkyl, characterized in that the process comprises the following steps: Step a) formation and recrystallization of the enantiomeric salt of formula (2), or solvate; Step b) recovery of the enantiomeric compound of formula (1) from its enantiomeric salt of formula (2) or solvate.

ARP150102373A 2014-07-31 2015-07-27 QUIRAL RESOLUTION OF THE ESTERS OF THE ACID 4-ARIL-2-TIAZOL-2-IL-1,4-DIHYDROPIRIMIDIN-5-CARBOXYL AR101319A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2014083385 2014-07-31

Publications (1)

Publication Number Publication Date
AR101319A1 true AR101319A1 (en) 2016-12-07

Family

ID=53761367

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150102373A AR101319A1 (en) 2014-07-31 2015-07-27 QUIRAL RESOLUTION OF THE ESTERS OF THE ACID 4-ARIL-2-TIAZOL-2-IL-1,4-DIHYDROPIRIMIDIN-5-CARBOXYL

Country Status (2)

Country Link
AR (1) AR101319A1 (en)
WO (1) WO2016016196A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR107633A1 (en) * 2016-02-19 2018-05-16 Hoffmann La Roche PROCEDURE FOR THE PREPARATION OF ACID 4-PHENYL-5-ALCOXICARBONIL-2-TIAZOL-2-IL-1,4-DIHYDROPIRIMIDIN-6-IL- [METHYL] -3-OXO-5,6,8,8A-TETRAHIDRO- 1H-IMIDAZO [1,5A] PIRAZIN-2-IL-CARBOXYL
US11247998B2 (en) 2017-07-27 2022-02-15 Jiangsu Hengrui Medicine Co., Ltd. Piperazine heteroaryl derivative, preparation method therefor and use of same in medicine
EP3732177B1 (en) 2017-12-28 2021-11-17 F. Hoffmann-La Roche AG Dihydropyrimidinylthiazole for the treatment and prophylaxis of hepatitis b virus infection
KR102732006B1 (en) 2019-03-25 2024-11-20 에프. 호프만-라 로슈 아게 Solid form of HBV core protein allosteric modulator compound

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10012823A1 (en) * 2000-03-16 2001-09-20 Bayer Ag New alkyl-6-aminoalkyl-dihydropyrimidine-5-carboxylate derivatives, useful for the treatment of viral, especially hepatitis B, infections
DE10125131A1 (en) * 2001-05-23 2002-12-05 Bayer Ag Process for the cleavage of the methyl 4- (2-chloro-4-fluorophenyl) -2- (3,5-difluoro-2-pyridinyl) -6-methyl-1,4-dihydro-5-pyrmidinecarboxylate racemate
CN100453542C (en) * 2007-04-30 2009-01-21 广东东阳光药业有限公司 Resolution method of 2-heterocyclic substituted dihydropyrimidine racemic compound
EP2892893B2 (en) * 2012-09-10 2019-10-16 F.Hoffmann-La Roche Ag 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection

Also Published As

Publication number Publication date
WO2016016196A1 (en) 2016-02-04

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