N-alkylation-intramolecular michael addition: New reaction manifold for high throughput annulation of amines

Calum MacLeod; Paul A. Tuthill; Roland E. Dolle

doi:10.1055/s-0029-1217962

N-alkylation-intramolecular michael addition: New reaction manifold for high throughput annulation of amines

Calum MacLeod, Paul A. Tuthill, Roland E. Dolle

Center for Drug Discovery

Research output: Contribution to journal › Article › peer-review

1 Scopus citations

Abstract

Parallel synthesis of -substituted pyrrolidines, piper-idines, morpholines, piperazines and diazaspirocycles was achieved in a single reaction step via the annulation of primary amines with halo-2-alkenyl esters, amides, nitriles and phenylsulfones.

Original language	English
Pages (from-to)	2857-2861
Number of pages	5
Journal	Synlett
Issue number	17
DOIs	https://doi.org/10.1055/s-0029-1217962
State	Published - 2009

Keywords

Amine
Annulation
Heterocycle
Intramolecular
Parallel synthesis

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10.1055/s-0029-1217962

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title = "N-alkylation-intramolecular michael addition: New reaction manifold for high throughput annulation of amines",

abstract = "Parallel synthesis of -substituted pyrrolidines, piper-idines, morpholines, piperazines and diazaspirocycles was achieved in a single reaction step via the annulation of primary amines with halo-2-alkenyl esters, amides, nitriles and phenylsulfones.",

keywords = "Amine, Annulation, Heterocycle, Intramolecular, Parallel synthesis",

author = "Calum MacLeod and Tuthill, {Paul A.} and Dolle, {Roland E.}",

year = "2009",

doi = "10.1055/s-0029-1217962",

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T1 - N-alkylation-intramolecular michael addition

T2 - New reaction manifold for high throughput annulation of amines

AU - MacLeod, Calum

AU - Tuthill, Paul A.

AU - Dolle, Roland E.

PY - 2009

Y1 - 2009

N2 - Parallel synthesis of -substituted pyrrolidines, piper-idines, morpholines, piperazines and diazaspirocycles was achieved in a single reaction step via the annulation of primary amines with halo-2-alkenyl esters, amides, nitriles and phenylsulfones.

AB - Parallel synthesis of -substituted pyrrolidines, piper-idines, morpholines, piperazines and diazaspirocycles was achieved in a single reaction step via the annulation of primary amines with halo-2-alkenyl esters, amides, nitriles and phenylsulfones.

KW - Amine

KW - Annulation

KW - Heterocycle

KW - Intramolecular

KW - Parallel synthesis

UR - http://www.scopus.com/inward/record.url?scp=70449379443&partnerID=8YFLogxK

U2 - 10.1055/s-0029-1217962

DO - 10.1055/s-0029-1217962

M3 - Article

AN - SCOPUS:70449379443

SN - 0936-5214

SP - 2857

EP - 2861

JO - Synlett

JF - Synlett

IS - 17

ER -

N-alkylation-intramolecular michael addition: New reaction manifold for high throughput annulation of amines

Abstract

Keywords

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