Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery

摘要

A library of macrocyclic compounds of the formula (I);where part (A) is a; bivalent radical, a —(CH2)y— bivalent radical or a covalent bond;where part (B) is a; bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond;where part (C) is a; bivalent radical, a —(CH2)t— bivalent radical, or a covalent bond; andwhere part (T) is a —Y-L-Z— radical wherein Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.

主权项

1. A compound of formula W-T-X, wherein W and X are independently selected from the group consisting of —OH and —NH2, and T is selected from the group consisting of:wherein
(W) indicates the site of a covalent bond to W and (X) indicates the site of a covalent bond to X; M is selected from the group consisting of —O—, —S—, —NH—, and —N(CH3)—; R10 and R11 are independently —H or —CH3; and n1, n2, n3, n4, n5, n6 and n7 are independently 1 or 2, andwherein the compound further comprises one or more protecting groups.