Method for the preparation of 4'-0-...

Details Method for the preparation of 4'-0-... Method for the preparation of 4'-0-...

C - Chemistry, Metallurgy

07

H

260/208.2

C07H 15/252 (2006.01)

Patent

CA 1289949

ABSTRACT OF THE DISCLOSURE For the preparation of 4'-0- tetrahydropyranyladriamycin b, the 9,14-position of the starting adriamycin is previously protected with phenyl- boronic acid and then the 4'-position of the thus protected adriamycin is selectively tetrahydropyranylated. After the tetrahydropyranylation, the by-product of 4'-0-tetrahydropyranyladriamycin a is converted to the aimed product of 4'-0- tetrahydropyranyladriamycin b. The yield of the product of 4'-0-tetrahydropyranyladriamycin b is high. The present invention provides a method for the preparation of 4'-0-tetrahydropyranyladriamycin b, where 3,4-dihydro-2H-pyran is added to a reaction solution containing a 9,14-protected adriamycin as obtained by (a) reacting adriamycin and phenyl-boronic acid or (b) reacting 4'-0-tetrahydropyranyladriamycin b and phenyl- boronic acid in the presence of an acid catalyst, for 4'- tetrahydropyranylation of the said 9,14-protected adriamycin, and then, the 9,14-protected position of the resulting product is deprotected and 4'-0- tetrahydropyranyladriamycin b is isolated by chromatography with silica-gel. - 13 -

522972

Affiliated with

Also associated with

Rating

Method for the preparation of 4'-0-... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Method for the preparation of 4'-0-..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Method for the preparation of 4'-0-... will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1266523