IP Library Granted Patent US 8,314,251
Granted Patent B2
US 8,314,251 · App. 13/184,356 · Granted Nov 20, 2012

Total synthesis of salinosporamide A and analogs thereof

Assignee: Nereus Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 8,314,251
App. No.
13/184,356
Granted
Nov 20, 2012
Kind
B2
Abstract

The present application relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs that includes forming a compound of formula (VIII).

Claims (7)

1. A compound of formula (VII):

wherein: R 1 is selected from the group consisting of hydrogen, an unsubstituted or substituted C 1-6 alkyl, and an unsubstituted or substituted aryl; and R 2 is selected from the group consisting of hydrogen, an unsubstituted or substituted C 1-6 alkyl, an unsubstituted or substituted aryl, and an unsubstituted or substituted arylalkyl.

2. The compound of claim 1 , wherein R 1 is an unsubstituted or substituted C 1-6 alkyl; and R 2 is an unsubstituted or substituted C 1-6 alkyl.

3. The compound of claim 1 , wherein R 1 is t-butyl; and R 2 is methyl.

4. The compound of claim 1 , having a structure selected from the group consisting of:

5. A method of preparing the compound of claim 1 comprising oxidizing the terminal double bond of the allyl substitutent at C-2 of a compound of formula (VI) to an aldehyde and reducing the aldehyde to a hydroxy group to form a compound of formula (VII):

wherein: R 1 is selected from the group consisting of hydrogen, an unsubstituted or substituted C 1-6 alkyl, and an unsubstituted or substituted aryl; and R 2 is selected from the group consisting of hydrogen, an unsubstituted or substituted C 1-6 alkyl, an unsubstituted or substituted aryl, and an unsubstituted or substituted arylalkyl.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 13, 2017
From: NEREUS PHARMACEUTICALS, INC.
To: TRIPHASE RESEARCH AND DEVELOPMENT I CORP.
Reel/Frame 041698/0404 →
Continuity (4)
Division 12399382 · Mar 6, 2009
Provisional Application 61034900 · Mar 7, 2008
Provisional Application 61073545 · Jun 18, 2008
Related Publication 20110269969A1 · Nov 3, 2011