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Title:
METHODS FOR MANUFACTURING BETULINIC ACID
Document Type and Number:
WIPO Patent Application WO2001051451
Kind Code:
A3
Abstract:
The present invention provides a method for preparing betulin-3-acetate including alcoholyzing betulin 3,28-dibenzoate; a process for preparing betulin-3-acetate including: (1) acylating betulin to provide betulin 3,28-dibenzoate and (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; and a process for preparing betulinic acid including: (1) acylating betulin to provide betulin 3,28-dibenzoate; (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; (3) oxidizing betulin-3-acetate to provide betulinic aldehyde-3-acetate; (4) oxidizing betulinic aldehyde-3-acetate to provide betulinic acid-3-acetate; and (5) deprotecting betulinic acid-3-acetate to provide betulinic acid.

Inventors:
KRASUTSKY PAVEL A (US)
CARLSON ROBERT M (US)
NESTERENKO VITALIY V (US)
Application Number:
PCT/US2001/000991
Publication Date:
March 07, 2002
Filing Date:
January 11, 2001
Export Citation:
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Assignee:
UNIV MINNESOTA (US)
KRASUTSKY PAVEL A (US)
CARLSON ROBERT M (US)
NESTERENKO VITALIY V (US)
International Classes:
C07C45/64; C07C47/46; C07C51/16; C07C51/235; C07C51/367; C07C62/06; C07C62/32; C07C69/00; C07C69/16; C07C67/29; (IPC1-7): C07C69/013; C07C67/08; C07C67/03; C07C67/29; C07C69/732; C07C67/39; C07C62/32; C07C51/367; C07C47/46; C07C45/64; C07C51/16; C07C69/00; C07J63/00
Domestic Patent References:
WO1998043936A21998-10-08
Foreign References:
EP0538189A21993-04-21
Other References:
L. F. TIETZE: "Synthesis of [13C]- and [2H]betulin for biological transformations", LIEBIGS ANNALEN DER CHEMIE, no. 12, December 1991 (1991-12-01), WEINHEIM DE, pages 1245 - 1249, XP002178263
YAO-CHANG XU: "A reagent for selective deprotection of alkyl acetates", JOURNAL OF ORGANIC CHEMISTRY, vol. 61, no. 26, 1996, EASTON US, pages 9086 - 9089, XP002178264
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