Process for preparing intermediates for a combinatorial dihydrobenzopyran library
AssigneePharmacopeia, Inc.
InventorsJohn J. Baldwin, John C. Reader, Lawrence W. Dillard, Ge Li, Jonathan J. Burbaum, Wenguang Zeng
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Abstract
Combinatorial libraries are disclosed which are represented by Formula I: (T'-L).sub.q -S-C(O)-L'-II' I wherein: S is a solid support; T'-L- is an identifier residue; and -L'-II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: ##STR1## which interact (i.e., as agonists or antagonists) with .alpha. adrenergic receptors, dopamine receptors, .sigma.-opiate receptors, and K.sup.+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.
Claims1
A process for preparing a compound of the formula ##STR600## where R.sup.2 is H or lower alkyl, said method comprising:
- a) reacting allyl 4-(hydroxymethyl)-3-nitrobenzoate with a compound of the formula ##STR601## in the presence of triphenylphosphine, toluene, and DEAD and stirring the mixture at room temperature to produce a compound of the formula ##STR602## wherein R is allyl;
- and b) reacting a compound so produced with methylene chloride, tetrakistriphenylphosphine palladium (0), and pyrrolidine and stirring the mixture at 0.degree. C.
Dependencies are inferred from the claim text.