Complex and structurally diverse compounds

A method for preparing a high-throughput screening library comprising:

• a) carrying out a ring expansion reaction, a ring fusion reaction, a ring rearrangement reaction, a ring cleavage reaction, or a combination thereof, on a natural product or a derivative thereof, wherein the natural product is quinine or a derivative thereof;
• b) carrying out an oxidation reaction, a reduction reaction, an esterification, an amidation, an addition reaction, a substitution reaction, an elimination reaction, an aromatization reaction, a functional group transformation, or a protection or deprotection reaction;
• optionally followed by carrying out an additional ring expansion reaction, a ring fusion reaction, a ring rearrangement reaction, or a ring cleavage reaction;
• and
• c) repeating steps a) and b) one to four times on the resulting products using different selections of reactions to provide a series of products for a high-throughput screening library;
• wherein the products comprise at least one ring distortion compared to the natural product;
• the products comprise at least three oxygen atoms, or at least two oxygen atoms and three nitrogen atoms;
• the products comprise at least two stereogenic centers, and the molecular weights of the products are at least about 400 Daltons and less than about 750 Daltons.