By Barry A. Bunin
ISBN-10: 0080542409
ISBN-13: 9780080542409
ISBN-10: 0121413403
ISBN-13: 9780121413408
Combinatorial chemistry has turn into an enormous concentration of study task for pharmaceutical, agrochemical, and biotechnology businesses. The explosion of combinatorial equipment has created the necessity for a compendium of trustworthy man made variations from the first literature. The Combinatorial Index fills this desire. integrated are chapters on linkers, solid-phase man made tools, analytical options, and resolution libraries. systems from the literature for developing combinatorial libraries of small molecules contain an crucial laboratory reference for the artificial chemist. each one method within the compilation is preceded by means of a bit entitled "Points of Interest," which highlights the strengths and boundaries of many of the tools. A structural appendix covers either useful workforce modifications and heterocyclization reactions in solid-phase synthesis. This finished yet easy-to-access consultant to the combinatorial chemistry literature will store time on tedious library searches, introduce a turning out to be viewers of chemists to this fascinating box, and decrease the limitations to trying a brand new or similar method.
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Extra info for The Combinatorial Index
Sample text
For Cleavage. The peptide polymer was treated with 2 mL of 30% H202 in 20 mL of acetic acid with stirring for 12 h at room temperature. 75 mmol of glycine (as the sodium salt) in a DMF/water solvent. The mixture was filtered and the filtrate was evaporated to dryness. 5, and the precipitate that formed was collected by decantation. The wet residue was dissolved in ethanol and evaporated to dryness. Protected peptides were further purified by recrystallization or chromatography. 9 1. Marshal, D.
Spear, K. L. Tetrahedron Lett. 1996, 37, 1145-1148. 2 PAL Linker: Fmoc-(Aminomethyl)-3,5-dimethoxyphenoxyvaleric Acid (PAL) Resin' Points of Interest 1. Support-bound amides were cleaved twice as fast from the PAL linker as the Rink linker (t~/24 min vs 9 min in 95/5 TFA/phenol). 2. The (aminomethyl)-3,5-dimethoxyphenoxyvaleric acid (PAL)linker was prepared from 4-hydroxy-2,6-dimethoxybenzaldehyde in five steps in 74 % overall yield. An efficient route to 4-hydroxy-2,6-dimethoxybenzaldehyde via the silyl-protected phenol has been reported by Landi and Ramig.
3 1. J. Org. Chem. 1994, 59, 79687975. 4 9-Xanthenyl (Xan) Linker: For Cleavage of Peptide Amides by Very Mild Acidolysis' Points of Interest 1. Sieber's Xan linker is more labile than the corresponding Rink amide linker: peptide amides were cleaved from the Xan resin with 98:2 dichloroethane/trifluoroacetic acid. 2. Cleavage from support was faster (<8 min) than aminolysis of sterically hindered peptide esters to provide peptide amides as described by Sheppard (see p 18). 3. The linker is prepared via a five-step sequence; it is also commercially available from a number of sources.
The Combinatorial Index by Barry A. Bunin
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