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.

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

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

SPOS Examples 6-9

Ugi 4CC (1)

SPOS Examples 6-10

Ugi 4CC (2)

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

SPOS Examples 6-12

Ugi 4CC (4)

SPOS Examples 6-13

Polymers as protective groups

SPOS Examples 6-14

Synthesis of Benzimidazoles (1)

SPOS Examples 6-15

Synthesis of Benzimidazoles (2)

SPOS Examples 6-16

Quinazolin-2,4-diones

SPOS Examples 6-17

Benzdiazepines

SPOS Examples 6-18

Pyrrolidines

SPOS Examples 6-19

Alcohol Attachment (1)

SPOS Examples 6-20

Alcohol Attachment (2)

SPOS Examples 6-21

Alcohol Attachment (3)

SPOS Examples 6-22

Cyclic (Thio-)Ureas (1)

SPOS Examples 6-23

Cyclic (Thio-)Ureas (2)

SPOS Examples 6-24

Purines (1)

SPOS Examples 6-25

Purines (2)

SPOS Examples 6-26

Quinolones

SPOS Examples 6-27

Pyridopyrimidines

SPOS Examples 6-28

1,3-dipolar Cycloaddition

SPOS Examples 6-29

SPOS Examples 6-30

1,3-dipolar Cycloaddition

SPOS Examples 6-31

Piperazines (1)

SPOS Examples 6-32

Piperazines (2)