IP Library › Granted Patent US 8,779,163
Granted Patent B2
US 8,779,163 · App. 13/420,108 · Granted Jul 15, 2014

Synthesis of UDP-Glucose:

Inventors: Bradford H. Hirth (Littleton, MA); Craig Siegel (Woburn, MA)
Assignee: Genzyme Corporation
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Quick Facts
Patent No.
US 8,779,163
App. No.
13/420,108
Granted
Jul 15, 2014
Kind
B2
Abstract

Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Claims (12)

1. A method of preparing a sphingosine-like compound represented by the following structural formula:

said method comprising the stop of reacting a cyclic starting material with HNR 2 R 3 ,said starting material represented by the following structural formula:

thereby forming an intermediate represented by the following structural formula:

and hydrolyzing the amino acetal group of the intermediate, thereby forming an acyclic compound represented by the following structural formula:

reacting the acyclic compound with an amide reducing agent, thereby forming an amine compound represented by the following structural formula:

debenzylating the —NHCH(—CH 2 OH)R 5 group of the amine compound, thereby forming a sphingosine-like compound represented by the following structural formula:

wherein:

R 1 is a substituted or unsubstituted aromatic group;

R 2 and R 3 are independently —H, a substituted or unsubstituted aliphatic group or, taken together with the nitrogen atom to which they art bonded, are a substituted or unsubstituted non-aromatic heterocyclie ring; and

R 5 is a substituted or unsubstituted aromatic group.

2. The method of claim 1 wherein the amine compound is debenzylated by hydrogenation.

3. The method of claim 2 wherein the amine compound is debenzylated by hydrogenation under a hydrogen atmosphere with a catalytic amount of a hydrogenation catalyst.

Continuity (6)
Division 12830962 · Jul 6, 2010
Continuation 11895632 · Aug 24, 2007
Division 10916824 · Aug 12, 2004
Division 10197227 · Jul 16, 2002
Provisional Application 60305814 · Jul 16, 2001
Related Publication 20120296088A1 · Nov 22, 2012