Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor

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Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor. / Giacoboni, Jessica; Clausen, Rasmus P.; Marigo, Mauro.

I: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis, Bind 27, Nr. 20, 12.2016, s. 2803-2806.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Harvard

Giacoboni, J, Clausen, RP & Marigo, M 2016, 'Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor', SYNLETT: Accounts and Rapid Communications in Chemical Synthesis, bind 27, nr. 20, s. 2803-2806. https://doi.org/10.1055/s-0036-1588313

APA

Giacoboni, J., Clausen, R. P., & Marigo, M. (2016). Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor. SYNLETT: Accounts and Rapid Communications in Chemical Synthesis, 27(20), 2803-2806. https://doi.org/10.1055/s-0036-1588313

Vancouver

Giacoboni J, Clausen RP, Marigo M. Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor. SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 2016 dec.;27(20):2803-2806. https://doi.org/10.1055/s-0036-1588313

Author

Giacoboni, Jessica ; Clausen, Rasmus P. ; Marigo, Mauro. / Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor. I: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 2016 ; Bind 27, Nr. 20. s. 2803-2806.

Bibtex

@article{2bb8629389f042ddaeb0252043936d18,
title = "Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor",
abstract = "A novel methodology for the synthesis of 3,3-difluoropiperidines has been developed. The target compounds are prepared in three steps using a robust protocol and simple starting materials. The incorporation of the fluorine is achieved by using the cheap and easily available ethyl 2-bromo-2,2-difluoroacetate as building block. Using this methodology, a new potent in vitro phosphodiesterase 2A (PDE2A) inhibitor containing the functionalized fluorinated piperidine scaffold has been prepared.",
keywords = "fluorine, piperidine, ethyl 2-bromo-2,2-difluoroacetate, reductive amination, phosphodiesterase",
author = "Jessica Giacoboni and Clausen, {Rasmus P.} and Mauro Marigo",
year = "2016",
month = dec,
doi = "10.1055/s-0036-1588313",
language = "English",
volume = "27",
pages = "2803--2806",
journal = "SYNLETT: Accounts and Rapid Communications in Chemical Synthesis",
issn = "0936-5214",
publisher = "Thieme",
number = "20",

}

RIS

TY - JOUR

T1 - Novel Approach toward 3,3-Difluoropiperidines from Easily Available Starting Materials and Synthesis of a New Phosphodiesterase Inhibitor

AU - Giacoboni, Jessica

AU - Clausen, Rasmus P.

AU - Marigo, Mauro

PY - 2016/12

Y1 - 2016/12

N2 - A novel methodology for the synthesis of 3,3-difluoropiperidines has been developed. The target compounds are prepared in three steps using a robust protocol and simple starting materials. The incorporation of the fluorine is achieved by using the cheap and easily available ethyl 2-bromo-2,2-difluoroacetate as building block. Using this methodology, a new potent in vitro phosphodiesterase 2A (PDE2A) inhibitor containing the functionalized fluorinated piperidine scaffold has been prepared.

AB - A novel methodology for the synthesis of 3,3-difluoropiperidines has been developed. The target compounds are prepared in three steps using a robust protocol and simple starting materials. The incorporation of the fluorine is achieved by using the cheap and easily available ethyl 2-bromo-2,2-difluoroacetate as building block. Using this methodology, a new potent in vitro phosphodiesterase 2A (PDE2A) inhibitor containing the functionalized fluorinated piperidine scaffold has been prepared.

KW - fluorine

KW - piperidine

KW - ethyl 2-bromo-2,2-difluoroacetate

KW - reductive amination

KW - phosphodiesterase

U2 - 10.1055/s-0036-1588313

DO - 10.1055/s-0036-1588313

M3 - Journal article

VL - 27

SP - 2803

EP - 2806

JO - SYNLETT: Accounts and Rapid Communications in Chemical Synthesis

JF - SYNLETT: Accounts and Rapid Communications in Chemical Synthesis

SN - 0936-5214

IS - 20

ER -

ID: 172089965