Gentles, Robert G. published the artcileStandardization Protocols and Optimized Precursor Sets for the Efficient Application of Automated Parallel Synthesis to Lead Optimization: A Mitsunobu Example, Recommanded Product: 3,3,3-Trifluoropropan-1-ol, the publication is Journal of Combinatorial Chemistry (2002), 4(5), 442-456, database is CAplus and MEDLINE.
Mitsunobu reactions of alcs. and phenols to give aryl alkyl ethers are optimized for automated parallel synthesis with potential use in lead optimization for drug discovery. Phenols are first selected to eliminate reactants with mol. weights > 210 g/mol, reactants with other potential reactive moieties which could interfere with biol. activity, labeled mols., reactants which might be incompatible with conditions for the Mitsunobu reaction, and reactants which are not com. available in multigram quantities from major vendors. Once the candidate phenols are selected, reactions of a set of alcs. with a single phenol substrate and reactions of a single alc. substrate with a variety of phenols are studied to compare the manual and automated versions of the Mitsunobu reaction. Both the automated and manual Mitsunobu reactions use di-tert-Bu azodicarboxylate (DBAD) and resin-bound triphenylphosphine as reagents. The resin-bound triphenylphosphine works best when exposure to air is minimized; in addition, use of resin-bound triphenylphosphine with consistent loading is important. With the automated and standardized methodol., a variety of aryl alkyl ethers are prepared
Journal of Combinatorial Chemistry published new progress about 2240-88-2. 2240-88-2 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Aliphatic hydrocarbon chain,Alcohol, name is 3,3,3-Trifluoropropan-1-ol, and the molecular formula is C3H5F3O, Recommanded Product: 3,3,3-Trifluoropropan-1-ol.
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