Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
View Patent ↗A library of macrocyclic compounds of the formula (I) where part (A) is a bivalent radical, a —(CH 2 ) y — bivalent radical or a covalent bond; where part (B) is a bivalent radical, a —(CH 2 ) z — bivalent radical, or a covalent bond; where part (C) is a bivalent radical, a —(CH2) t — bivalent radical, or a covalent bond; and where part (T) is a —Y-L-Z— radical wherein Y is CH 2 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.
1. A compound of formula W-T-X, wherein W and X are independently selected from the group consisting of —OH and —NH 2 , 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(CH 3 )—;
R 10 and R 11 are independently —H or —CH 3 ; and
n 1 , n 2 , n 3 , n 4 , n 5 , n 6 and n 7 are independently 1 or 2, and
wherein the compound further comprises one or more protecting groups.
2. A compound having one of the following structures: