Patent ID: 7235578
Filing Date: 2007-06-26
Classification: A61K,A61P,C07D,Y02A

Abstract:
1. A process of preparing a compound of formula (I) wherein A and B together may represent a fused optionally substituted benzene and a fused optionally substituted naphthalene, where the optional substituents are represented by Y; wherein Y is selected from one or more of H, a halogen, CH X is halogen or OSO W is further selected from the group wherein J is selected from OH or R wherein R represents H, lower C P is a group which is a substrate suitable for a nitroreductase or carboxypeptidase enzyme such that one of said enzymes is able to bring about the removal of the group P which is selected from the following moieties: wherein each occurrence of Z′ is independently H or CH wherein E is selected from —N═, or —CH═, G is O, S, or NH, Q is either (a) absent or independently selected from one to three of R, —OR, halogen, —NRR, —NO (CH or a fused group; where R represents H, lower C HET may represent a 5- or 6-membered carbocycle or heterocycle containing one or two atoms independently selected from N, O and S; or a physiologically functional derivative thereof, wherein the process for preparing a compound of formula I comprises the steps of (a) converting the NO wherein the variables A, B, and Y are as defined above in this claim, (b) converting a compound of formula (II′) by allylation of the NHBOC groups into a compound of formula (III′) wherein the variables A, B, and Y are as defined above in this claim, (c) converting a compound of formula (III′) into an indole derivative of formula (IV′) wherein the variables A, B, and Y are as defined above, (d) reacting the compound of Formula (IV′) in the presence of Zn powder to give a compound of Formula (V′) wherein the variables A, B, and Y are as defined above in this claim, and (e) reacting the NBOC and allyl groups of Formula (V′) as desired to give a compound of Formula (I) wherein the variables A, B, Y, W, and Z are as defined above.