COMBINED PRODUCTION PROCESS FOR LIBRARY OF AMIDE, CARBAMATE AND SULFONAMIDE USING SCAVENGER

摘要

PROBLEM TO BE SOLVED: To obtain an amide library containing plural variable substituent groups useful for discovering a medicine efficiently and in high yield by using a scavenger in a solution phase. SOLUTION: A scavenger is used in a solution phase when a compound having an amide skeleton containing three variable substituent groups is produced. Each library compound is produced in a different reaction part, the library compound is a compound of formula I (R1 and R2 are H or a noninhibitory substituent group; R3 is a noninhibitory group). (i) an (n) equivalent of a solvent-soluble primary amine or secondary amine reagent of formula II is added to each reaction part containing a liquid medium, (ii) 1.1n equivalent of an acyl halide of the formula R3 C(O)X(X is a halogen) and a neutralizing base are added to the reaction part of the process (i), (iii) a scavenger of formula III [(p) is an insoluble solid retainer; L is a bifunctional bond group; (am ine ) is a primary substituent group, etc.], is added to each reaction part of the process (ii) and (iv) the scavenger is separated from each reaction part and each purified amide library compound is recovered.