Efficient syntheses of zoledronic acid as an active ingredient of a drug against osteoporosis

Dávid Illés Nagy, A. Grün, Krisztina Lévay, Sándor Garadnay, István Greiner, G. Keglevich

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

The reaction of 1H-imidazol-1-ylacetic acid and two equivalents of phosphorus trichloride/phosphorous acid at 75 °C in sulfolane, or in the presence of catalytic amounts of [bmim][BF4] afforded zoledronic acid in yields up to 75%. The joint use of the ionic liquid additive and sulfolane as the solvent was synergetic affording highly valuable zoledronic acid in a record yield of 93%.

Original languageEnglish
Pages (from-to)663-671
Number of pages9
JournalSynthetic Communications
Volume48
Issue number6
DOIs
Publication statusPublished - Mar 19 2018

Fingerprint

zoledronic acid
Ionic Liquids
Pharmaceutical Preparations
Acids
sulfolane

Keywords

  • 1H-imidazol-1-ylacetic acid
  • ionic liquid additive
  • P-reagents
  • sulfolane
  • synthesis
  • zoledronic acid

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Efficient syntheses of zoledronic acid as an active ingredient of a drug against osteoporosis. / Nagy, Dávid Illés; Grün, A.; Lévay, Krisztina; Garadnay, Sándor; Greiner, István; Keglevich, G.

In: Synthetic Communications, Vol. 48, No. 6, 19.03.2018, p. 663-671.

Research output: Contribution to journalArticle

Nagy, Dávid Illés ; Grün, A. ; Lévay, Krisztina ; Garadnay, Sándor ; Greiner, István ; Keglevich, G. / Efficient syntheses of zoledronic acid as an active ingredient of a drug against osteoporosis. In: Synthetic Communications. 2018 ; Vol. 48, No. 6. pp. 663-671.
@article{b7b04ee2785d4b4297fcede67dc3c427,
title = "Efficient syntheses of zoledronic acid as an active ingredient of a drug against osteoporosis",
abstract = "The reaction of 1H-imidazol-1-ylacetic acid and two equivalents of phosphorus trichloride/phosphorous acid at 75 °C in sulfolane, or in the presence of catalytic amounts of [bmim][BF4] afforded zoledronic acid in yields up to 75{\%}. The joint use of the ionic liquid additive and sulfolane as the solvent was synergetic affording highly valuable zoledronic acid in a record yield of 93{\%}.",
keywords = "1H-imidazol-1-ylacetic acid, ionic liquid additive, P-reagents, sulfolane, synthesis, zoledronic acid",
author = "Nagy, {D{\'a}vid Ill{\'e}s} and A. Gr{\"u}n and Krisztina L{\'e}vay and S{\'a}ndor Garadnay and Istv{\'a}n Greiner and G. Keglevich",
year = "2018",
month = "3",
day = "19",
doi = "10.1080/00397911.2017.1410894",
language = "English",
volume = "48",
pages = "663--671",
journal = "Synthetic Communications",
issn = "0039-7911",
publisher = "Taylor and Francis Ltd.",
number = "6",

}

TY - JOUR

T1 - Efficient syntheses of zoledronic acid as an active ingredient of a drug against osteoporosis

AU - Nagy, Dávid Illés

AU - Grün, A.

AU - Lévay, Krisztina

AU - Garadnay, Sándor

AU - Greiner, István

AU - Keglevich, G.

PY - 2018/3/19

Y1 - 2018/3/19

N2 - The reaction of 1H-imidazol-1-ylacetic acid and two equivalents of phosphorus trichloride/phosphorous acid at 75 °C in sulfolane, or in the presence of catalytic amounts of [bmim][BF4] afforded zoledronic acid in yields up to 75%. The joint use of the ionic liquid additive and sulfolane as the solvent was synergetic affording highly valuable zoledronic acid in a record yield of 93%.

AB - The reaction of 1H-imidazol-1-ylacetic acid and two equivalents of phosphorus trichloride/phosphorous acid at 75 °C in sulfolane, or in the presence of catalytic amounts of [bmim][BF4] afforded zoledronic acid in yields up to 75%. The joint use of the ionic liquid additive and sulfolane as the solvent was synergetic affording highly valuable zoledronic acid in a record yield of 93%.

KW - 1H-imidazol-1-ylacetic acid

KW - ionic liquid additive

KW - P-reagents

KW - sulfolane

KW - synthesis

KW - zoledronic acid

UR - http://www.scopus.com/inward/record.url?scp=85041914939&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85041914939&partnerID=8YFLogxK

U2 - 10.1080/00397911.2017.1410894

DO - 10.1080/00397911.2017.1410894

M3 - Article

AN - SCOPUS:85041914939

VL - 48

SP - 663

EP - 671

JO - Synthetic Communications

JF - Synthetic Communications

SN - 0039-7911

IS - 6

ER -