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Library Synthesis 6-1 Combi Chem: letzter Block http://pubs.acs.org/isubscribe/journals/cen/81/i19/html/8119s ci2.html THE SMALL-MOLECULE APPROACH TO BIOLOGY http://pubs.acs.org/isubscribe/journals/cen/81/i09/html/8109ge nomics.html Steven V. Ley's group at the University of Cambridge carried out the first total synthesis of the bioactive alkaloid (+)-plicamine (Image 4) [Angew. Chem. Int. Ed., 41, 2194 (2002 ); C&EN, June 17, page 26 ]. All transformations used in the synthesis were done with supported reagents and scavengers, avoiding the need for any chromatographic, crystallization, or distillation steps.
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Combi Chem: letzter Block

Feb 08, 2022

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Page 1: Combi Chem: letzter Block

Library Synthesis 6-1

Combi Chem: letzter Block•http://pubs.acs.org/isubscribe/journals/cen/81/i19/html/8119sci2.html

•THE SMALL-MOLECULE APPROACH TO BIOLOGY http://pubs.acs.org/isubscribe/journals/cen/81/i09/html/8109genomics.html

•Steven V. Ley's group at the University of Cambridge carried out the first total synthesis of the bioactive alkaloid(+)-plicamine (Image 4) [Angew. Chem. Int. Ed., 41, 2194 (2002); C&EN, June 17, page 26]. All transformations used in the synthesis were done with supported reagents and scavengers, avoiding the need for any chromatographic, crystallization, or distillation steps.

Page 2: Combi Chem: letzter Block

Library Synthesis 6-2

Dynamic CombinatorialChemistry

•http://pubs.acs.org/isubscribe/journals/cen/80/i50/html/8050chemhighlights2.html

•Update Combi Chem

•http://pubs.acs.org/isubscribe/journals/cen/80/i45/html/8045combinatorial.html

Page 3: Combi Chem: letzter Block

Library Synthesis 6-3

Library Synthesis

•Multicomponent one-pot reactions

•Multigeneration reactions

•Liquid-liquid phase extraction (LPE)

•Liquid-solid phase extractions (SPE) using polymeric scavengers

•Solution reactions using polymer-bound reagents or catalysts

Page 4: Combi Chem: letzter Block

SPOS Examples 6-9

Ugi 4CC (1)

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SPOS Examples 6-10

Ugi 4CC (2)

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SPOS Examples 6-11

Ugi 4CC (3)

Zu einer Lösung von 0.42 mmol Aldehyd in 0.5 ml Me0H wirdeine Lösung von 0.42 mmol Säure, 0.42 mmol Isonitril und 0.42 mmol Amin (methanolische Lösung) in 1.5 ml Me0Hzugetropft. 65 Stdn. bei Raumtemp. rühren

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SPOS Examples 6-12

Ugi 4CC (4)

Page 8: Combi Chem: letzter Block

SPOS Examples 6-13

Polymers as protective groups

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SPOS Examples 6-14

Synthesis of Benzimidazoles (1)

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SPOS Examples 6-15

Synthesis of Benzimidazoles (2)

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SPOS Examples 6-16

Quinazolin-2,4-diones

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SPOS Examples 6-17

Benzdiazepines

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SPOS Examples 6-18

Pyrrolidines

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SPOS Examples 6-19

Alcohol Attachment (1)

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SPOS Examples 6-20

Alcohol Attachment (2)

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SPOS Examples 6-21

Alcohol Attachment (3)

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SPOS Examples 6-22

Cyclic (Thio-)Ureas (1)

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SPOS Examples 6-23

Cyclic (Thio-)Ureas (2)

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SPOS Examples 6-24

Purines (1)

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SPOS Examples 6-25

Purines (2)

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SPOS Examples 6-26

Quinolones

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SPOS Examples 6-27

Pyridopyrimidines

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SPOS Examples 6-28

1,3-dipolar Cycloaddition

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SPOS Examples 6-29

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SPOS Examples 6-30

1,3-dipolar Cycloaddition

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SPOS Examples 6-31

Piperazines (1)

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SPOS Examples 6-32

Piperazines (2)