Solid-Phase library synthesis of alkoxyprolines

Journal of Combinatorial Chemistry

Volumn 3, Issue 4, 2001, Pages 367-373

  Boldi, Armen M ^a   Dener, Jeffrey M ^a   Hopkins, Thutam P ^a  

^a Discovery Partners International   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DRUG DERIVATIVE; DYES, REAGENTS, INDICATORS, MARKERS AND BUFFERS; PROLINE; PROTEINASE INHIBITOR;

ALKYLATION; ARTICLE; CHEMISTRY; COMBINATORIAL CHEMISTRY; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; SYNTHESIS; ULTRAVIOLET SPECTROPHOTOMETRY;

ALKYLATION; COMBINATORIAL CHEMISTRY TECHNIQUES; INDICATORS AND REAGENTS; MAGNETIC RESONANCE SPECTROSCOPY; PROLINE; PROTEASE INHIBITORS; SPECTROPHOTOMETRY, ULTRAVIOLET;

EID: 0035407227     PISSN: 15204766     EISSN: None     Source Type: Journal    
DOI: 10.1021/cc010007s     Document Type: Article

References (29)

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24. 2 and examined. Any color change to a dark color indicates free thiophenol. With free thiophenol resin, the beads will turn dark green-black. The test will indicate no free phenol if no color change from the original resin color is observed. This is not a quantitative test but a qualitative measure of resin loading.
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27. The limit of detection for free phenol was determined by adding known quantities of unacylated Marshall resin to a functionalized sample. Additional amounts of unacylated Marshall resin were added until a postive test for phenol was obtained by the ferric chloride test.
28. Library analysis was performed by flow injection MS for identity of 12.5% of library wells. For each library, six reference samples were analyzed by LC-MS for qualitative purity (area under the curve by UV at 214 nm and evaporative light scattering detection) and subjected to a weight percent purity analysis. The weight percent purity analysis is a method for quantifying the amount of product in a production library well. Several compounds were purified to homogeneity. Standard detection curves for HPLC-UV were made for these purified and characterized standards to represent the diversity of the chemistry within the library. Compounds of the same structure found in the production library were sampled from the expected positions. The absolute mass of the product as determined by HPLC divided by mass recovery for a given well gave the weight percent purity.
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