Synthesis of an H3 Antagonist via Sequential One-Pot Additions of a Magnesium Ate Complex and an Amine to a 1,4-Ketoester followed by Carbonyl-Directed Fluoride Addition-Reference-Cited by-同舟云学术

Synthesis of an H3 Antagonist via Sequential One-Pot Additions of a Magnesium Ate Complex and an Amine to a 1,4-Ketoester followed by Carbonyl-Directed Fluoride Addition

Published:2012-08-06 Issue:8 Volume:16 Page:1393-1403
ISSN:1083-6160
Container-title:Organic Process Research & Development
language:en
Short-container-title:Org. Process Res. Dev.

Author:

Hawkins Joel M.¹,Dubé Pascal¹,Maloney Mark T.¹,Wei Lulin¹,Ewing Marcus¹,Chesnut Stephen M.¹,Denette Joshua R.¹,Lillie Brett M.¹,Vaidyanathan Rajappa¹

Affiliation:

1. Pharmaceutical Sciences, Pfizer Inc., Eastern Point Road, Groton, Connecticut 06340, United States

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/op300093j

Reference40 articles.

1. Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor

2. Therapeutic potential of histamine H3 receptor agonists and antagonists

3. Involvement of histamine in the control of the waking state

4. Discovery of Two Clinical Histamine H3 Receptor Antagonists: trans-N-Ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-Fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764)

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