AR052879A1 - PROCEDURE TO PREPARE BETA DERIVATIVES CHIRAL AMINO ACIDS BY ASYMMETRIC HYDROGENATION - Google Patents

PROCEDURE TO PREPARE BETA DERIVATIVES CHIRAL AMINO ACIDS BY ASYMMETRIC HYDROGENATION

Info

Publication number
AR052879A1
AR052879A1 ARP060100175A AR052879A1 AR 052879 A1 AR052879 A1 AR 052879A1 AR P060100175 A ARP060100175 A AR P060100175A AR 052879 A1 AR052879 A1 AR 052879A1
Authority
AR
Argentina
Prior art keywords
procedure
amino acids
asymmetric hydrogenation
chiral amino
prepare beta
Prior art date
Application number
Other languages
Spanish (es)
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
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR052879A1 publication Critical patent/AR052879A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invencion se refiere a un procedimiento para la preparacion eficiente de derivados de beta aminoácidos enriquecidos enantioméricamente que son utiles en la síntesis asimétrica de moléculas biologicamente activas. El procedimiento comprende una hidrogenacion enantioselectiva de un sustrato derivado de beta aminoácido acrílico proquiral en presencia de una sal de amonio y un precursor de metal de transicion complejado con un ligando de ferrocenil difosfina quiral.The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives that are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a substrate derived from beta prokyl acrylic amino acid in the presence of an ammonium salt and a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.

ARP060100175 2005-01-24 2006-01-17 PROCEDURE TO PREPARE BETA DERIVATIVES CHIRAL AMINO ACIDS BY ASYMMETRIC HYDROGENATION AR052879A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US64669705P 2005-01-24 2005-01-24

Publications (1)

Publication Number Publication Date
AR052879A1 true AR052879A1 (en) 2007-04-11

Family

ID=36587261

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060100175 AR052879A1 (en) 2005-01-24 2006-01-17 PROCEDURE TO PREPARE BETA DERIVATIVES CHIRAL AMINO ACIDS BY ASYMMETRIC HYDROGENATION

Country Status (8)

Country Link
EP (1) EP1856028A1 (en)
JP (1) JP2008528503A (en)
CN (1) CN101175714A (en)
AR (1) AR052879A1 (en)
AU (1) AU2006208297A1 (en)
CA (1) CA2594494A1 (en)
TW (1) TW200637805A (en)
WO (1) WO2006081151A1 (en)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009084024A2 (en) 2007-11-02 2009-07-09 Glenmark Generics Limited A process for the preparation of r-sit agliptin and its pharmaceutically acceptable salts thereof
CN102271504B (en) 2008-12-31 2014-08-20 凯瑞斯德股份有限公司 Process and intermediates for the preparation of n-acylated-4-aryl beta-amino acid derivatives
EP2223923A1 (en) 2009-02-25 2010-09-01 Esteve Química, S.A. Process for the preparation of a chiral beta aminoacid derivative and intermediates thereof
IT1395596B1 (en) 2009-06-30 2012-10-16 Dipharma Francis Srl PROCEDURE FOR THE PREPARATION OF SITAGLIPTIN
CZ303113B6 (en) 2010-03-16 2012-04-11 Zentiva, K.S. Process for preparing sitagliptin
EP2547682A1 (en) 2010-03-31 2013-01-23 Teva Pharmaceutical Industries Ltd. Solid state forms of sitagliptin salts
US8765668B2 (en) 2010-06-04 2014-07-01 Lek Pharmaceuticals D.D. Methods of synthesis of β-aminobutyryl substituted compounds
EP2392575A1 (en) 2010-06-04 2011-12-07 LEK Pharmaceuticals d.d. A novel synthetic approach to ß-aminobutyryl substituted compounds
EP2397141A1 (en) 2010-06-16 2011-12-21 LEK Pharmaceuticals d.d. Process for the synthesis of beta-amino acids and derivatives thereof
EP2609099A2 (en) 2010-08-27 2013-07-03 USV Limited Sitagliptin, salts and polymorphs thereof
WO2012035549A2 (en) 2010-09-13 2012-03-22 Panacea Biotec Ltd An improved process for the synthesis of beta amino acid derivatives
EP2508506A1 (en) 2011-04-08 2012-10-10 LEK Pharmaceuticals d.d. Preparation of sitagliptin intermediates
EP2527320A1 (en) 2011-05-27 2012-11-28 LEK Pharmaceuticals d.d. Preparation of Sitagliptin Intermediates
EA024688B1 (en) 2011-07-27 2016-10-31 ФАРМА ДжРС, Д.О.О. Process for the preparation of sitagliptin and its pharmaceutically acceptable salts
WO2013065066A1 (en) 2011-11-02 2013-05-10 Cadila Healthcare Limited Processes for preparing 4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro [l,2,41-triazolo[43-a]pyrazin-7(8h)-yl]-l-(2,4,5- trifluorophenyl)butan-2-amine
EP2615080A1 (en) 2012-01-12 2013-07-17 LEK Pharmaceuticals d.d. Preparation of Optically Pure ß-Amino Acid Type Active Pharmaceutical Ingredients and Intermediates thereof
EP2674432A1 (en) 2012-06-14 2013-12-18 LEK Pharmaceuticals d.d. New synthetic route for the preparation of ß aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-alpha]pyrazin-7-yl compounds
US9227901B2 (en) * 2012-07-05 2016-01-05 Abbvie Inc. Process for preparing bicyclic amine derivatives
CN102898387B (en) * 2012-09-26 2015-01-07 浙江工业大学 Channelized method for continuously producing N-[(2Z)-piperazine-2-subunit]-2, 2, 2-trifluoroacetyl hydrazine
CN105315286B (en) * 2014-07-30 2018-08-17 连云港润众制药有限公司 The preparation of Xi Gelieting
KR102359436B1 (en) * 2015-06-05 2022-02-09 (주)아모레퍼시픽 Methods for manufacturing methyl 2-propyl-6-(trifluoromethyl) nicotinate
CN105254519B (en) * 2015-11-25 2017-05-17 常州吉恩药业有限公司 Synthesizing method of sitagliptin key intermediate
EP3424927B1 (en) 2017-07-04 2019-04-17 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid
CN107325025B (en) * 2017-07-17 2019-04-09 中国科学院化学研究所 A kind of chiral alpha-amino acid derivatives and preparation method thereof
CN113636950B (en) * 2020-05-11 2023-01-17 浙江医药股份有限公司新昌制药厂 Preparation method of chiral 4-aryl-beta-amino acid derivative
WO2024121301A1 (en) 2022-12-09 2024-06-13 Krka, D.D., Novo Mesto Process for the preparation of sitagliptin

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE59408655D1 (en) * 1993-10-01 1999-09-30 Novartis Ag Ferrocenyldiphosphines substituted with fluoroalkyl as ligands for homogeneous catalysts
AR043515A1 (en) * 2003-03-19 2005-08-03 Merck & Co Inc PROCEDURE TO PREPARE CHIRAL DERIVATIVES BETA AMINO ACIDS BY ASYMMETRIC HYDROGENATION
TW200602293A (en) * 2004-04-05 2006-01-16 Merck & Co Inc Process for the preparation of enantiomerically enriched beta amino acid derivatives

Also Published As

Publication number Publication date
CN101175714A (en) 2008-05-07
CA2594494A1 (en) 2006-08-03
TW200637805A (en) 2006-11-01
AU2006208297A1 (en) 2006-08-03
EP1856028A1 (en) 2007-11-21
WO2006081151A1 (en) 2006-08-03
JP2008528503A (en) 2008-07-31

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