Biomedical Engineering Reference
In-Depth Information
TABLE 5.21 Representative Examples of Homosilatecan Library 88
Entry
R
1
R
2
Product, Yield (%)
1
(CH
2
)
2
CF
3
H
88a
,42
2
n
-Bu
F
88b
,35
3
Me
CF
3
88c
,49
4
Me
OAc
88d
,29
5
n
-Bu
NHBoc
88e
,26
SCHEME 5.33
Synthesis of 24 homosilatecan analogs by parallel deprotections.
5.6 CONCLUSIONS
Over the past decade, the synthesis of chemical libraries has matured from a pure
enumeration to a consideration of compound quality, including chemical diversity
and scaffold novelty. While libraries composed of individual, pure samples vs.
mixture libraries are inherently more difficult, expensive, and slower to prepare,
steady advances in automated synthesis, purification, and analysis are still greatly
expediting access to high-quality compound collections. This includes technologies
such as microwave reactors, flow chemistry, solid-phase and split-pool synthesis
strategies, as well as polymer-linked reagents and dynamic combinatorial library
