High quality libraries require highly optimized reactions. Could one of your chemists optimize these reactions and prepare a library of single compounds in one week? .^L\
θ © —Phe— Rink—-
Ala —Phe—Rink
R1R2NH/Na(CN)BH3
\
X N«.-
©
'&
TFA/H20
Phe—NH?
\ Ala—Phe—Rink
(Cleavage)
#
Ro
0 Q 0 Q
Ri
Rink amide forming handle. Pyridinium dichromate. N, N-Dimethylformamide. Trifluoroacetic acid.
The two-step reaction sequence shown above was fully optimized and a small library of 50 single compounds prepared by one chemist in less than one week using Multipin Technology™ and SynPhase™ crowns. This included the three-step synthesis of the model proline system. The library size can be increased by a factor of 10-100 in a similar time scale, with the extra time required for reagent preparation being the only limiting factor. The table below gives examples of representative compounds and conversions.
Hi Amine R 1 R 2 NH
% Target Compound HPLC(214nm)*
5-Amino-2-methoxypyridine 2-Amino-1 -propanol 4-Bromoaniline 3,4-Dihydroxybenzylamine 2,2-Diphenylethylamine 3-Methoxyaniline Piperidine
92 90 92 93 94 95 88
:
::
*Overall conversion including preparation of proline model.
SynPhase crowns and Multipin technology are synonymous with reaction optimization. The combination has the following advantages: ik Rapidity * Cost effective. ik Allows multiple parallel syntheses. ik Is able to handle diverse reaction conditions. Ά Permits multiple cleavage of individual compounds. ~fc The compounds are presented in a format suitable for high throughput analysis and testing. Ά The modular format facilitates compound tracking. Ά Requires no weighing. Ά" R e q u i r e s n o f i l t r a t i o n .
Multipin™ technology using SynPhase™ crowns make rapid and efficient optimizations possible. Contact us today for details of your nearest distributor or to obtain full information on how you can achieve similar productivity gains. HIRON
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